Download CBCS Pharmaceutical Chemistry20 09-10 OUCW

1
(CBCS APPLIED TO M.Sc PHARMACEUTICAL CHEMISTRY)
DEPARTMENT OF CHEMISTRY
OU. COLLEGE FOR WOMEN
OSMANIA UNIVERSITY
(Effective from academic year 2009-2010)
Semester 1
S.No
1.
2.
3.
4.
5.
6
7.
8.
Paper
title
Paper-I (core)
Ph.Chem 101
Paper-I I(core)
Ph.Chem 102
Paper-III (core)
Ph.Chem 103
Paper-I V(core)
Ph.Chem 104
Paper-V (core)
Ph.Chem 105
Pharma.Chem Lab
(Core)
Ph.Chem 151
Pharma.Chem Lab
(Core)
Ph.Chem 152
Pharma.Chem Lab
(Core)
Ph.Chem 153
Instruction
Hrs/week
4
Duration of
examination
3
Internal
Assessment
20marks
Semester
exam
80marks
Total
Marks
100marks
Credits
4
3
20marks
80marks
100marks
4
4
3
20marks
80marks
100marks
4
4
3
20marks
80marks
100marks
4
4
3
20marks
80marks
100marks
4
6
6
-
75
75 marks
3
6
6
-
75
75 marks
3
6
6
-
75
75 marks
3
725 marks
29
Total
4
2
Semester 2
S.No
1.
2.
3.
4.
5.
6
7.
8.
Paper
title
Paper-I (core)
Ph.Chem 201
Paper-II (core)
Ph.Chem 202
Paper-III (core)
Ph.Chem 203
Paper-I V(core)
Ph.Chem 204
Paper-V (core)
Ph.Chem 205
Pharma.Chem Lab
(Core)
Ph.Chem 251
Pharma.Chem Lab
(Core)
Ph.Chem 252
Pharma.Chem Lab
(Core)
Ph.Chem 253
Instruction
Hrs/week
4
Duration of
examination
3
Internal
Assessment
20marks
Semester
exam
80marks
Total
Marks
100marks
Credits
4
3
20marks
80marks
100marks
4
4
3
20marks
80marks
100marks
4
4
3
20marks
80marks
100marks
4
4
3
20marks
80marks
100marks
4
6
6
-
75
75 marks
3
6
6
-
75
75 marks
3
6
6
-
75
75 marks
3
725 marks
29
Total
4
3
Semester 3
S.No
1.
2.
3.
4.
5.
6
7.
8.
Paper
title
Paper-I (core)
Ph.Chem 301
Paper-II (core)
Ph.Chem 302
Paper-I II(core)
Ph.Chem 303
Paper-I V(core)
Ph.Chem 304
Paper-V
(Interdisciplinary)
ID/ Ph.Chem305/
pool-3
Seminar
Pharma.Chem Lab
(Core)
Ph.Chem 351
Pharma.Chem Lab
(Core)
Ph.Chem 352
Pharma.Chem Lab
(Core)
Ph.Chem 353
Instruction
Hrs/week
4
Duration of
examination
3
Internal
Assessment
20marks
Semester
exam
80marks
Total
Marks
100marks
Credits
4
3
20marks
80marks
100marks
4
4
3
20marks
80marks
100marks
4
4
3
20marks
80marks
100marks
4
4
3
20marks
80marks
100marks
4
2
6
6
-
75
25marks
75 marks
1
3
6
6
-
75
75 marks
3
6
6
-
75
75 marks
3
750 marks
30
Total
4
Semsester 4
S.No
1.
6
7.
Paper
title
Paper-I
(Interdisciplinary)
ID/ Ph.Chem401/
pool-3
Seminar
Pharma.Chem Lab
(Core)
Ph.Chem 451
PROJECT
WORK
Instruction
Hrs/week
4
Duration of
examination
3
Internal
Assessment
20marks
Semester
exam
80marks
Total
Marks
100marks
Credits
2
6
6
-
75
25marks
75 marks
1
3
15
(DESERTATION
AND VIVA
VOCE)
Total
-
-
-
100marks
4
300
marks
2500
12
Grand total marks and credits
4
100
4
SYLLABUS
FOR
M.Sc. PHARMACEUTICAL CHEMISTRY
I – IV SEMESTERS
From 2009-10 Onwards
OSMANIA UNIVERSITY
HYDERABAD
5
M.Sc PHARMACEUTICAL CHEMISTRY
SEMESTER-I
PAPER- I( Ph.C 101): BASICS OF PHARMACEUTICAL CHEMISTRY
Ph.C-01
Statistical validation.
Ph.C-02
Rheology
Ph.C-03
Physical pharmacy
Ph.C-04
Introduction to pharmaceutics, Dissolution and Disintegration
PAPER- II(Ph.C 102): PHARMACEUTICAL INORGANIC AND
ANALYTICAL CHEMISTRY
Ph.C-05: Limit tests and Inorganic pharmaceuticals
Ph.C-06: Micromeritics and Physicochemical characterization of pharmaceutical solids
Ph C-07: Titrimetric analysis
Ph.C-08: Electro chemical analysis
PAPER-III (Ph.C 103): REAGENTS AND REACTION MECHANISMS IN
PHARMACEUTICAL SYNTHESIS
Ph.C-09: Nucleophilic Substitution Reactions
Ph.C-10: Elimination reactions and reaction pathways
Ph.C-11: Reagents in pharmaceutical synthesis - I
Ph.C-12: Nitrogen Heterocycles
PAPER-IV (Ph.C 104): SPECTROSCOPY-1
Ph.C-13: General principles of spectroscopy
Ph.C-14: Principles of IR spectroscopy and applications.
Ph.C-15: Principles of UV Spectroscopy and applications.
Ph.C-16: Proton NMR and simplification techniques
PAPER-V (Ph.C105): MATHEMATICS AND COMPUTER APPLICATIONS
Ph.C-17: Mathematics
Ph.C-18: Statistics
Ph.C-19 : Computer Applications
Ph.C-20 : Quantum Chemistry.
PRACTICALS:
PAPER-VI (Ph.C–151): SYNTHESIS OF ORGANIC PHARMACEUTICALS &
INTERMEDIATES
PAPER-VII (Ph.C-152): PHARMACEUTICAL ANALYSIS-I
PAPER-VIII (Ph.C-153): INSTRUMENTAL ANALYSIS
6
SEMESTER-II
PAPER-I(Ph.C 201): SYNTHETIC PHARMACEUTICALS & BIOMOLECULES
Ph.C-21:
Ph.C-22:
Ph.C-23:
Ph.C-24:
Reagents in pharmaceutical synthesis – II
Synthetic pharmaceuticals
Protiens and Vitamins
Nucleic acids and Recombinant DNA Technology
PAPER-II(Ph.C- 202): SPECTROSCOPY-II
Ph.C-25: C-13 NMR, 2D- NMR & Qualitative and quantitative applications
of H1 NMR
Ph.C-26: Mass spectrometry
Ph.C-27: Advanced techniques and Applications of Mass Spectrometry
Ph.C-28: Principles and pharmaceutical applications of AAS, AES and
Spectroflorimetry
PAPER –III(Ph.C –203): BIOPHARMACEUTICAL CHEMISTRY AND DYNAMICS
Ph.C-29: Fermentation Technology
Ph.C-30: Enzymes and Biotransformations
Ph.C-31: Drug Interactions
Ph.C-32: Pharmacodynamics
PAPER -IV (Ph.C-204)
Ph.C-33:
Ph.C-34:
Ph.C-35:
Ph.C-36:
Herbal Drugs
Alkaloids
Glycosides and Prostaglandins
Steroids and Hormones
PAPER -V (Ph.C-205)
Ph.C-37:
Ph.C-38:
Ph.C-39:
Ph.C-40:
NATURAL PHARMACEUTICALS
CHIROTECHNOLOGY
Optical isomerism
Chirality & Biological activity
Conformational isomerism & biological effects
Assymmetric synthesis
PRACTICALS:
PAPER-VI (Ph.C-251):
QUALITATIVE ANALYSIS OF ORGANIC COMPOUNDS
& PHARMACEUTICALS.
PAPER- VII (Ph.C- 252): PHARMACEUTICAL ANALYSIS
PAPER -VIII (Ph.C- 253): INSTRUMENTAL ANALYSIS
7
SEMESTER III
PAPER-I (Ph.C-301): CHEMISTRY OF PHARMACOLOGY
Ph.C-41: CNS Depressants,stimulants,
Cholinergic, Adrenergic agonists and antagonists
Ph.C-42: Cardiovascular agents and Hematological agents
Ph.C-43: Chemotherapeutics
Ph.C-44: Gastro intestinal agents, Diuretics, Anti inflammatory agents
PAPER-II (Ph.C- 302): PHARMACOKINETICS AND THERAPEUTICS
Ph.C-45: Pharmacokinetics – I
Ph.C-46: Pharmacokinetics – II
Ph.C-47: Principles of Therapeutics
Ph.C-48: Drug delivery Systems.
PAPER-III (Ph.C-303): ANALYSIS BY SEPARATION TECHNIQUES
Ph.C-49: Applications of solvent extraction and Principles of
Chromatography
Ph.C-50: Gas chromatography ,GC-MS and GC-FTIR
Ph.C-51: HPTLC, HPLC and HPLC-MS
Ph.C-52: Size-exclusion chromatography, Capillary electrophoresis,
Super Critical fluid Chromatography, Ultra Performance
Liquid Chromatography
PAPER-IV(Ph.C-304): PHARMACEUTICAL DESIGN AND DEVELOPMENT
Ph.C-53:
Ph.C-54:
Ph.C-55:
Ph.C-56:
PAPER-V (ID-305):
ID-1
ID-2
ID-3
ID-4
Principles Of Drug Discovery & SAR studies
QSAR Studies
Molecular Modeling
Modeling Biomolecules
CBCS (Interdisciplinary paper)
PRACTICALS:
PAPER VI–(Ph.C-351): QUALITATIVE ANALYSIS OF ORGANIC MIXTURES& QSAR
STUDIES OF KNOWN BIOLOGIALLY ACTIVE SERIES
PAPER-VII(Ph.C- 352): SYNTHESIS OF ORGANIC PHARMACEUTICALS &
ISOLATION OF HERBAL DRUGS.
PAPER-VIII(Ph.C- 353):CHROMATOGRAPHY AND SPECTRAL ANALYSIS OF
PHARMACEUTICALS.
8
SEMESTER - IV
PAPER-I(ID- 401 ): CBCS
ID-1
ID-2
ID-3
ID-4
PRACTICALS:
Paper-II (Ph.C- 451): QUANTITATIVE ANALYSIS OF PHARMACEUTICALS
Paper-III (Ph.C- 452): PROJECT / DESSERTATION WORK
9
M.Sc Pharmaceutical Chemistry
I semester syllabus (From 2008onwards)
A. Theory Course
PAPER- I( Ph.C 101): BASICS OF PHARMACEUTICAL CHEMISTRY
Ph.C-01
Ph.C-02
Ph.C-03
Ph.C-04
Statistical validation.
Rheology
Physical pharmacy
Introduction to pharmaceutics, Dissolution and disintegration
Ph.C-01 Statistical validation.
Errors in pharmaceutical analysis : Introduction, classification, accuracy, precision, minimization
of systemic errors. Statistical validation- Statistical treatment of finite examples( mean, median,
average deviation, standard deviation, coefficient variation and variance calculations).
Distribution of random numbers. Significant figures- computation rules. Comparison of results
(students t-test, variance-ratio test or f-test), method of least squares. Correlation Coefficient,
rejection of result-Q test.
Ph.C-02 Rheology
Introduction, concept of viscosity, kinematic viscosity, mechanism of enhanced viscosity, factors
influencing viscosity-intrinsic and extrinsic factors. Newtonian flow, non-Newtonian flow.
Thixotropy, negative thixotropy, Rheopexy & measurement of thixotropy. Determination of
rheological properties(flow properties).Selection of viscometers. Newtonian flow – Ostwald
viscometer, falling sphere viscometer. Non Newtonian flow – cup & bob viscometer & cone &
plate viscometer. Viscoelasity (introduction only), psychorheology & applications to pharmacy.
(problems to be discussed wherever necessary)
Ph.C-03 Physical pharmacy
Physical properties of drug molecules: Dielectric constant, Induced polarization, refractive
index, molar refraction , optical rotation .
Buffered and isotonic solutions: Buffer equation, common ion effect, buffer equation for weak
acid and its salt and weak base and its salt. Factors influencing PH of buffer solutions. Drugs as
buffers. PH of indicators,buffer capacity and its calculations, Van Slyke equation, influence of
concentration on buffer capacity and maxin buffer capacity.
Buffers in pharmaceutic and
biological system- in vivo biologic buffer systems, pharmaceutical buffers and their preparation.
Influence of buffer capacity and PH on tissue irritation, stability vs. optimum therapeutic
response. pH and solubility. Buffered isotonic solution, measurement of toxicity. Calculating
toxicity and methods of adjusting toxicity and PH.
10
Ph.C-04: Introduction to pharmaceutics, Dissolution and disintegration
Introduction to I.P, B.P & USP monographs.Introduction to pharmaceutical dosage formsDefinition and requirement for formulation of pharmaceuticals. Classification of dosage forms.
Dissolution: Drug absorption, theories of drug dissolution – Diffusion layer model, Danckwert’s
model & interfacial barrier model. Factors influencing dissolution, dissolution tests for tablets
and capsules (basket apparatus, paddle apparatus, flow through cell apparatus). In vitro- in vivo
correlation of dissolution.Disintegration tests for tablets, capsules and enteric coated tablets.Solid
dosage forms: Tablets-Classification. Properties of tablets, evaluation of tablets.
Capsules..Liquid dosage forms: monophasic-for internal and external use, Monophasic-Syrups,
Elixirs. Biphasic: Emulsions(various types), stability and evaluation of emulsions. Suspensions:
Flocculated and nonflocculated systems, evaluation of suspensions Semisolid dosage forms:
Suppositories. Ointments: Special types and evaluation, Creams.,Parenterals, Injectables
Recommended text books :
1. Practical pharmaceutical chemistry. By A.H.Backette, J.B.Stenlake, Part-A & B.
2. Pharmaceutical analysis by Ashtoshkar
3. Fundamentals of analytical chemistry by Skoog & West
4. Physical Pharmacy by AN.Martin,J, Swarlbick etal
5. Physical pharmaceutics by Shotton and Ridgeway
6. Text book of Physical Phamacy by Hadkar
7. Text book of physical pharmaceuticals by Subramaniyan
8. Essentials of Physical chemistry and pharmacy by Arnikar & Kadam
9. Introduction to pharmaceuticals by Mittal
10. Pharmaceutical dosage forms and drug delivery systems by Ansel
11. Introduction to Pharmaceuticals by Gupta, Volume I & II.
12. Modern pharmaceutics by Banker and Rhode
References:
1.
2.
3.
4.
British Pharmacopoeia vol I,II
Indian Pharmacopoeia vol I,II
Bently’s Text book of pharmaceutics by Rowlins
The science and practice of pharmacy by Remington
11
PAPER- II(Ph.C 102):PHARMACEUTICAL INORGANIC AND
ANALYTICAL CHEMISTRY
Ph.C-05: Limit tests and Inorganic pharmaceuticals
Ph.C-06: Micromeritics and Physicochemical characterization of pharmaceutical
solids
Ph.C-07: Titrimetric analysis
Ph.C-08: Electro chemical analysis
Ph.C-05 : Limit tests and Inorganic pharmaceuticals:
Limit tests for insoluble matter, limit tests of soluble matter, limits of moisture, volatile matter,
residual matter, residual solvents, limits of nonvolatile matter, limits of residue on ignition, limits
of loss on ignition, limits on ash value( for above all explain with 1 example). Limit tests for
metallic impurities: lead, arsenic, iron: Limit tests for acid radical impurities, chlorides, sulfates,
arsenate, carbonate, cyanide, oxalate, phosphate.Limit tests for nonmetallic impurities: Boron,
free Halogens, Selenium.
Inorganic pharmaceuticals : i)Antioxidants : Introduction, criteria for action as anti oxidants,
mechanism of action. Preparation, properties and assay of hypophosphorus acid ii) Topical
agents: Introduction, categories ,protectives and adsorbents, silicone polymers, antimicrobials
and hydrogen peroxide. iii) Astringents: alum
iv) Dental products. Introduction, anticaries agents-sodium flouride, dentifriers-dibasic calcium
phosphate. v) Inhalants: Introduction, role of oxygen, carbon dioxide and ammonia, nitrous oxide
as inhalant. vi) Intra cellular and extra cellular electrolytes- body fluid compartments, role of
major physiological cations and anions, sodium chloride.
Ph.C-6: Micromeritics and Physicochemical characterization of Pharmaceutical solids
Introduction, particle size analysis- concepts of particle size, size distribution, mean size of
particulate system, methods of particle size analysis (sieving, microscopic method, sedimentation
methods, electrical sensing zone method, optical sensing zone and light diffraction method).
X-ray Diffraction studies: Polymorphism, Weiss coefficients, Miller indices, Bragg’s equation.
Experimental methods- the rotating crystal method, oscillating crystal method, powder method,
indexing the reflections, systemic absences and applications.
Thermal methods: Thermogravimetry- Theory, Instrumentation, Methodology and
applications.Differential thermal analysis- theory, Instrumentation, Methodology and
applications.Thermometric
titrationsTheory,
Instrumentation,
Methodology
and
applications.Differential scanning calorimetry - Theory, Instrumentation, Methodology and
applications.
Ph.C-7: Titrimetric analysis:
Introduction to titrimetry: Acid -base titrations, Titration curves, systemic equilibrium
calculations, theory and selection of indicators. Non-aqueous titrartions- theory, eg. Assay of
aspirin. Precipitation titrations: Solubility product, titration curves, determination of end points.
Formation of a soluble colored compound, use of adsorption indicators. eg. Determination of
chloral hydrate in dichlorophenazine
Redox titrations: Electrode potentials, Nernst equation, formal potentials, titration curves.
Feasibility of redox titrations, types and selection of redox indicators,eg. Assay of ascorbic acid,
12
Complexometric titrations: Stability of complexes, titration curves, metal ion indicatorsProperties and theory. Types of EDTA titrations. Titration of mixture. eg: Determination of
calcium gluconate in calcium gluconate injection
Ph.C-8: Electro chemical analysis
Theory,
reference electrodes- calomel electrode, silver-silver chloride electrode,
mercury(I)sulphate electrode, salt bridges. Indicator electrode-Hydrogen, glass, redox electrodes.
Ion selective electrode- glass membrane electrode, crystalline membrane electrode, liquid
membrane electrode, gas diffusion membrane electrode. Potentiometric titrations.
eg. Nitrazepam and allopurinol. ( working of problems wherever necessary)
Amperometry: Introduction, theory, instrumentation (dropping mercury electrode), rotating
platinum electrode, twin polarised microelectrodes)
eg. Procainamide hydrochloride.
Polarography: Theory, current, voltage, curve, half wave potential, instrumentation, applications.
Recommended text books:
1. Vogel’s text book of quantitative chemical analysis
2. Quantitative analysis by Day & Underwood
3. Pharmaceutical analysis By Chapman
4. Pharmaceutical analysis By Ashtoshkar
5. Analytical chemistry by open learning by Clive Whatson
6. Physical chemistry by Atkins
7. Physical chemistry by Glasstone
8. Solid state chemistry by West
9. Instrumental methods of analysis by Willard
10. Inorganic pharmaceutical chemistry By Chatwal
11. Inorganic pharmaceutical chemistry By Mohammadali
12 Inorganic pharmaceutical and medicinal chemistry By Quadri and Quadri
13.Practical pharmaceutical chemistry Part I by Beckett & Stenlake
14. Physical pharmacy by AN.Martin,J,Swarlbick etal
15. Text book of physical pharmaceuticals by CVS Subramaniyan
Rreferences
1. Practical pharmaceutical chemistry. By A.H.Backette, J.B.Stenlake.
2. British Pharmacopoeia vol I,II
3. Indian Pharmacopoeia vol I,II
4. Fundamentals of analytical chemistry. By Skoog and West.
5. Pharmaceutical analysis. By Takeru,Higuchi
6. .Pharmaceutical analysis By. David G.Watson
7. Bently’s Text book of pharmaceutics by Rowlins
8. The science and practice of pharmacy by Remington
13
PAPER-III(Ph.C 103): REAGENTS AND REACTION MECHANISMS IN
PHARMACEUTICAL SYNTHESIS
Ph.C-9: Nucleophilic Substitution Reactions
Ph.C-10: Elimination reactions and reaction pathways
Ph.C-11: Reagents in pharmaceutical synthesis
Ph.C-12: Nitrogen Heterocyclics
Ph.C-9: Nucleophilic Substitution Reactions:
A brief review of nucleophilic substitution reactions at saturated carbon:SN1,SN2 and Snimechanisms and stereochemistry-Factors affecting SN1 and SN2 mechanisms- nature of
structure, nucleofuse, nucleophile and solvent.
Ambient nucleophiles-Definition and types,NGP by n, Pi, sigma electrons.
Aromatic nucleophilic substitutions(SNAr): SN1(Ar),SN2(Ar) and Benzyne mechanismsEvidence.. Aliphatic electrophilic substitution- SE1,SE2 and SEi mechanism-Evidence.
Ph.C-10: Elimination reactions and reaction pathways:
Elimination reactions : Definition and Classification - -Eleminations. E2; E1; and E-1cB
mechanisms - Orientation of double bonds in elimination reactions - Zaitsev Vs Hoffman
products. Pyrolytic eleiminations : Ei - mechanism
Reaction Pathways. Kinetic and non-Kinetic methods of determination - order of reaction,
molecularity, transition states, energy profile daigrams, primary and secondary kinetic isotopic
effetcs. Isolation and characterization of products and intermediates - Cross over experiments Isotopic labelling studies - Spectral studies of the reactions and reaction intermediates.
Ph.C-11:Reagents in pharmaceutical synthesis-I
1.Reducing agents: catalytic hydrogenation , sodium borohydride, lithium aluminium hydride
and sodium/alcohol. Modified Hydride reagents: Lithium boro hydride, lithiumdiisopropyl
amide, Sodium cyanoborohydride, sodium triacetoxy boro hydride,Diisobutyl aluminium
hydride . Application to the reduction of alkenes, alkynes, carbonyl and azo compounds. 2.
Reduction of nitro compounds in acid, base and neutral media.Oxidizing agents: Sulfuric acid,
Potassium permanganate, osmium tetroxide, chromium trioxide and peracids . Application to
the oxidation of alkenes, alkynes alcohols and carbonyl compounds with one example each.
Ph.C-12: Nitrogen Heterocyclics
Pyridine: Synthesis-Hantsch synthesis & from 1,5-dicarbonyl compounds. and reactions with
electrophiles, nulceophiles
and
oxidation reactions.
Synthesis of
pyridine based
pharmaceuticals : Isoniazid. Quinoline: Synthesis-Skraup & Combes synthesis and reactions
with electrophiles, nucleophiles and oxidizing agents, and reducing agents.. Structures of
chloroquine .
isoquinoline: Synthesis-Bischler –Napieralski synthesis, Pictet –Splenger synthesis, and
reactions with electrophiles, nucleophiles and oxidizing agents, and reducing agents.. Structures
of chloroquine
Indoles: Synthesis-Fisher Indole synthesis,Bischler synthesis, and reactions with electrophilic
reagents, nucleophilic reagents, oxidising agents, and reducing agents..
14
Diazines: Synthesis-from 1,4 dicarbonyl compounds, 1,3 dicarbonyl compounds,& from 1,2 di
ketones, and reactions of- pyridazine, pyrimidine and pyrazine;
Recommended text books:
1. Advanced Organic Chemistry. By Jerry March
2. Mechanism and structure in Organic Chemistry. By Gould
3. TextBook of Organic chemistry. By Graham Solomons
4. TextBook of Organic Chemistry. By Loudon
5. Organic reaction mechanisms. By Ingould
6. Reaction mechanisms. By Agarwal
7. Textbook of Organic chemistry. By Morrison and Boyd
8. Organic reaction mechanisms. By Ahluwalia
9. Medicinal chemistry. By Chatwal.
10. Medicinal chemistry. By Ashtoshkar.
11. Heterocyclic chemistry by Joule and Smith
12. Heterocyclic chemistry by Acheson
13. Heterocyclic chemistry by Bansal
References:
1. Reactions,Rearrangements and Reagents. By Sanyal & Sanyal
2. Chemistry of Drugs. By V.N.Ivers.
3. May’s chemistry of synthetic drugs. Hand Book of Reagents for organic synthesis. By
Reich,Rigby
4. Hand book of reagents for organic synthesis:oxidising & reducing agents. By Burk
.
15
PAPER-IV(Ph.C 104): SPECTROCOPY
Ph.C-13:
General principles of spectroscopy
Ph.C-14:
Principles of IR spectroscopy and applications.
Ph.C-15:
Principles of UV Spectroscopy and applications.
Ph.C-16:
Proton NMR and simplification techniques.
Ph.C-13: General principles of spectroscopy
Introduction to specroscopy. characterization of electromagnetic radiation ( problems associated
). Atomic specra- Atomic emission, atomic absorption. Molecular spectrum- absorption,
emission (Jablonsky diagram), regions of electromagnetic spectrum. Instrumentation- Basic
elements of spectrometers- light sources, monochromators, cells, detectors and read out systems.
Spectrophotometers- single beam, double beam. Representation of spectra, Width of specral
lines- collision broadening, Doppler broadening. Heisenberg uncertainity. Intensity of spectral
lines - transition probability, population of states and path length of the sample.
Ph.C-14: Principles of IR spectroscopy and applications:
Principle, Vibrational energy levels of diatomic molecules, selection rules. Calculation of force
constatnt anharmonic nature of vibrations, normal modes of vibrations. Concept of group
frequencies, instrumentation (dispersive and FTIR) Characteristic vibrational frequencies of
functional groups, structural and stereochemical effects on absorption pattern in carbonyl group,
in substituted benzenes, cis- trans isomerism , H- bonding, tautomerism and conformational
analysis. Quantitative applications of IR: Measurement of absorbance-baseline method,
calibration graph method, standard addition method. Eg: Determination of amount of
phenobarbitone in phenobarbitone tablets, determination of the amount of acetyl salicylic acid
and phenacetin .
Ph.C-15: Principles of UV Spectroscopy and applications:
Introduction to UV spectroscopy, Beer-Lambert’s law. Electronic energy levels of molecules,
selection rules for electronic spectra. Instrumentation. Types of electronic transitions in organic
molecules, Chromophores: conjugated dienes, trienes and polyenes, unsaturated carbonyl
compounds. Woodward-Fieser rules-benzene and its derivatives, polynuclear aromatic
hydrocarbons, diketones. Solvent and structural influences on absorption maxima,
stereochemical factors: angular strain, steric hindrance, cis-trans isomers, angular distortion and
cross conjugation. Quantitative applications of UV: Use of standard absorptivity value, use of
calibration graph, single point and double point standardisation. Assay of substances in
multicomponent samples - assay as a single component sample. Assay after solvent
extraction,assay after correction for interference, simultaneous equation method.Eg. Flusemide
in tablet form, mixture of pethidine hydrochloride and chlorocresol. Difference
spectrophotometry- analysis of aspirin in dextropropoxyphene compound tablets.
Ph.C-16: Proton NMR and simplification techniques:
Magnetic susceptibility. principles of magnetic resonance, magnetic moment and spin angular
moment. Larmour frequency, magnetic resonance (H1,C13,B11,F19,P31,N15), instrumentation.
Shielding constants, chemical shifts, shielding and deshielding mechanisms, spin-spin coupling
and coupling constants. application of PMR spectroscopy in structure determination. Electro
negativity, Keto-enol tautomerism, proton exchange in alcohols, amines and carboxylic acids,
16
hydrogen bonding, C-N rotation.Simplification technics of H1 NMR-Double resonance, Proton
decoupling, High field strength,NOE and use of chemical shift reagents.
Recommended text books :
1.
2.
3.
4.
5.
6.
7.
Fundamentals of spectroscopy by Banwell
Practical pharmaceutical chemistry by Beckett & Stenlake
Fundamentals of analytical chemistry by Skoog & West
Atomic structure and chemical bond by Manaschanda
Orgaic spectroscopy by William Kemp
Organic spectroscopy by Kalsi
Introduction to spectroscopy by Pavia
References.
1. Spectroscopic identification of Organic Compounds. By Silverstein, Basseler & Morri
2. Instrumental methods of analysis by B.K.Sharma
3. Instrumental methods of analysis by Chatwal & Anand
4. British open university monograph
5. Organic spectroscopy by Jagmohan
6. Pharmaceutical analysis by Watson
7. Vogel’s quantitative chemical analysis
8. Analytical profiles of drugs
9. Analytical chemistry by Christian
17
PAPER-V (Ph.C105): MATHEMATICS AND COMPUTER APPLICATIONS
Ph.C-17:
Ph.C-18:
Ph.C-19:
Ph.C-20:
Mathematics
Statistics
Computer Applications
Quantum Chemistry
Ph.C-17: Mathematics
Co-ordinate system:-Graphical representation of the functions:
Y=ex,y=lnx, y=kx2 , y=sin x, y=cos x, y=tan x.
ii. Differential Calculus-Functions – continuity and differentiability.Rules for
differentiation.Sums,products and quotients of functions . The chain rule. Differentiation of
algebraic, exponential, logarithmic & composite functions.Higher order derivatives. Maxima and
minima. Partial differentiation& Meaning of total derivative.Exact and inexact differentials.
Integral calculus-Basic rules for integration, Methods for evaluating integrals – the substitution
method, use of partial fractions, integration by parts. Definite integrals.
Elementary
differential
equations:First
order
differential
equations
–seperable
variables,homogeneous and linear differential equations. Linear second order differential
equations- solution of the homogeneous equation.
Ph.C-18: Statistics:
i.Permutations and combinations. Probability, laws of probability. Addition and multiplication of
probabilities.Distribution of sample means, measurement control charts, number defective
control charts.
ii.Significance tests: Null hypothesis, comparison of variability- F-test(related problems),
comparison of means- t-tests(related problems),, comparison of frequencies- 2 (chisquare)
test(related problems).
iiRegression analysis – Linear Regression, Multi linear regression – non linear regression.
Ph.C 19: Computers for chemists:
Introduction to computers (Input and Output devices, central processing unit) software and computer
languages. Algorithms and flow charts.
C language instructions. Constants, variables and key words. Operators in C-arithemic, relation,
logical and address operators. If and If-else statements. Loops- While loop and For loop. C language
functionsprintf( ), scanf ( ), getsf ( ), and putsf ( )Arrays, pointers and functions. Steps in testing a source
program in C.
C-language Programmes for:a. Roots of a quadratic equation
b. First-order rate constant from kinetic data
c. Summation of series
d. Least- square fitting of X-Y data to a straight line.
e. Calculation of activation energy using Arrhenius equation by least-square fitting.
f. Calculation of energy as a function of entire nuclear separation for H2+ ion.
g. Dissociation constant of acetic acid from conductance data.
h. Values at different x for a particle in a one-dimensional box.
18
Ph.C 20: QUANTUM CHEMISTRY
The Originof Quantum Mechanics. The Failures of classical physics- Black Body radiation,
Plank Distribution, Heat Capacities, Atomic and Molecular Spectra.Wave Particle Duality-The
Particle nature of Electromagnetic Radiation (Photoelectric Effect), The Wave Character of
Particles (De Broglies Equation). The Diffraction of Electrons. The Dynamic of Microscopic
Function- The Schrodinger Equation, The Born interpretation of the wave equation
(Normalisation and Quantisation).
Quantum meachinical Principles- The information in a wave function (The probability density,
Eigen Values, Eigen function. Operators,Super position and expectation values
The Uncertainity Principle.
References:
1.
2.
3.
4.
5.
6.
7.
8.
9.
10.
11.
12.
13.
14.
15.
Let us C By Yashwant Khanitkar
Basic programming By Balaguruswamy
Basic programming Schaum series
Computer fundamentals By Balaguruswamy
Computer fundamentals By Hunt and Shelley
Mathematical preparation for Physical Chemistry, F. Daniels, McGraw Hill
Mathematics for Chemistry, Doggett and Sutcliffe, Longman
Mathematics for Chemists, D.M. Hirst, MacMillan
The science and practice of pharmacy Vol-I By Remington
Fundamentals of mathematics and statstics for students of chemistry
i. and allied subjects. By C.J.Brrokes.
Atkin`s Physical chemistry by Peter Atkins and Julio de Paula
Physical chemistry by Ira N.Levin
Physical chemistry- A molecular approach by DA McQuarrie and J.D Simon
Molecular thermodynamics by DA McQuarrie and J.D Simon
Introduction to Quantum chemistry by AK.Chandra
19
=====================================================================
====
B. LABORATORY COURSES:
PAPER-VI (Ph.C–151):
INTERMEDIATES
SYNTHESIS
OF
ORGANIC
PHARMACEUTICALS
&
Synthesis of organic pharmaceuticals and intermediates: 1.m-Dinitro benzene, 2 Acetanilide, 3.
p-nitro acetanilide, 4. m-nitro aniline 5.Aspirin 6.Paracetamol 7.Phenytoin 8. Florescène
9.Chloritone 10. Azalactone 11. Umbelliferone 12. 2-substituted Benzimidazole
Preparation of Pharmaceutical formulations:
1.Sulpha ointment 2.Benadryl syrup 3.. Salicylin ointment.
PAPER-VII (Ph.C-152): PHARMACEUTICAL ANALYSIS-I
Limit tests: for chloride, sulphate, phosphate, iron, Lead and Arsenic in inorganic and organic
pharmaceuticals
Assay of Pharmaceuticals
Calibration of weights, pipettes and burette.
Assay of Aspirin, Codiene phopsphate ( Acid-base titrations )
Assay of chloride in Ringers lactate (Precipitation titrations)
Assay of phenolic group in Organic pharmaceuticals
PAPER-VIII (Ph.C – 153): INSTRUMENTAL ANALYSIS
Tests for hardness of tablets , Friability, Disintegration tests for uncoated, coated and enteric
coated tablets, capsules.
Colorimetric estimation of Ascorbic acid
Colorimetric estimation of dextrose in dextrose injection
Conductometric assay of pharmaceuticals
Qualitative analysis of pharmaceuticals by IR spectroscopy.
20
M.Sc Pharmaceutical Chemistry
II - Semester Syllabus
A. Theory Course
PAPER-I(Ph.C 201): SYNTHETIC PHARMACEUTICALS & BIOMOLECULES
Ph.C-21:
Reagents in pharmaceutical synthesis – II
Ph.C-22:
Synthetic pharmaceuticals
Ph.C-23:
Protiens and Vitamins
Ph.C-24: Nucleic acids and Recombinant DNA Technology
Ph.C-21: Reagents in pharmaceutical synthesis-II
Organao –metallic reagents – Preparation and aspplication of the following in organic and
pharmaceutical synthesis with mechanism- Grignard reagent, organo lithium, organo boron
reagent( Hydroboration , reaction of organoborane in C-C bond formation), Organo silicon
reagents & utility of trialkyl silyl halide, trialkyl silyl cyanide and trialkyl silyl triflate.
Protecting groups-Principles of protection of alcohols-ether, ester formation. Protection of
amines- acetylation, benzoylation, benzyloxy carbonyl and triphenyl methyl groups. Protection
of carbonyl groups-acetal, ketal,1,2-glycols and 1,2-dithioglycol formation.
Ph.C-22: Synthetic pharmaceuticals
Synthesis and pharmacological activity of the following drugs. Benzocaine (local anaesthetic),
Phenobarbitone, Nitrazepam (hypnotic), Diclofenac, celecoxib, (anti-inflammatory),
Pheniramine(anti-histamine), Enalapril (anti-hypertensive), Isoprenalin (sympathomimetic),
procainamide (cadio-vascular) and omeprazole (anti-ulcer).
Synthesis and pharmacological activity of the following drugs:- Cis-Platin, 5-FluoroUracil (anticancer),
Tinidazole
(anti-amoebic),
Miconazole
(anti-fungal),
Ciprofloxacin,
norfloxacin(antibacterials), Ethambutal Anti-tubercular), Clofazimine (anti-leprosy and antiT.B.), Cloxacillin, Cephalexin (anti-biotics) and Lamivudine(anti- AIDs).
Ph.C-23: Proteins & Vitamins:
Introduction to proteins, color reactions, molecular weight determination. Classification into
simple, conjugated and derived proteins. Peptide linkage, primary structureof proteins, Cterminal aminoacid determination, N-terminal amino acid determination. Partial hydrolysis.
Determination of primary structure. Synthesis of peptides by various mehods. Spacial
arrangement of protein molecule. Classification of proteins. Secondary and tertiary and
quarternary structure of proteins.
Vitamins: Definition, occurrence, structural formulae and physiological functions of vitaminsA1(Retinol 3,7-dimethyl-9-(2,6,6-trimethyl-1-cyclohexen-1-yl)-2,4,,6,8-nonatetraene-1ol),A2(3,4 didehydro rotenol),B1(Thiamine),B2(Riboflavin),B6(Pyridoxin), Nicotinic acid , B12
(cyanocobalamine (5,6-dimethyl benzimidazolyl cyanocobamide) and vitamin C(Ascorbic
21
acid),D2 ( Calciferol,-9,10-secoergosta-5,7,10(19),22-tetraene-3-ol) ,E (Tocopherol) and
K(Phylloquinone).
Ph.C-24: Nucleic acids and Recombinant DNA Technology
Structure of the bases- Adenine, Thiamine, Guanine ,Uracil and cytosine. Structure and synthesis
of nucleosides and nucleotides. Structure of DNA and RNA. Conformational structures of
nucleic acids. Synthesis of oligonucleotides, sequencing of DNA. Replication, transcription and
translation. Genetic code as a means to protein synthesis. Biosynthesis of proteins and
importance of heredity
Recominant DNA Technology - Introduction; restriction enzymes, recombinant DNA technolgy
using plasmids, phase and cosmids; Polymerase chain reaction- principle, components technique
method, Sanger’s method automated DNA sequencing . Applications - Insulin, human growth
hormone, vaccines, interferons, novel enzymes.
Recommended text books:
1.
2.
3.
4.
5.
6.
7.
Organic reaction mechanisms By Ahluwalia
Reaction mechanisms. By Agarwal
Reactions,Rearrangements and Reagents. By Sanyal & Sanyal
Hand Book of Reagents for organic synthesis. By Reich,Rigby
Hand book of reagents for organic synthesis. Auxallaries: By Coates.
Hand book of reagents for organic synthesis. Protecting groups: By Pearson.
Hand book of reagents for organic synthesis:oxidising & reducing agents. By Burk
References:
1. Chemistry of Drugs. By V.N.Ivers.
2. May’s chemistry of synthetic drugs. By G.M.Dyar
3. The organic chemistry of Drug synthesis.vol 1-6 By Ledneicer etal.
4. Top Drugs: The synthetic routes. J.Saunders.
5. Medicinal chemistry. By Chatwal.
6. Medicinal chemistry. By Ashtoshkar.
7. Biochemistry. By Lehninger.
8. Biochemistry. By Stryer.
9. Biochemistry. By Rastogi.
10. Biochemistry. By Chatwal.
11. Biochemistry. By Well.
12. Organic Chemistry by McMurray
13. The Biochemistry of the Nucleic acids By Adams,Knowler and Leader
22
PAPER-II(Ph.C- 202): SPECTROSCOPY- II
Ph.C-25: C13 NMR , 2D- NMR & Qualitative and quantitative
applications of H1 NMR
Ph.C-26: Mass spectrometry
Ph.C-27: Advanced techniques and Applications of Mass
Spectroscopy
Ph.C-28: Principles and pharmaceutical applications of AAS , AES and
Spectroflorimetry
Ph.C-25: C13 NMR , 2D NMR & Qualitative and quantitative applications of H1 NMR:
Recording C13 NMR spectra -undecoupled, proton decoupled, off-resonance decoupled and
selective proton decoupled spectra. C13 chemical shift data- structural, electronic and steric
effects on chemical shifts. Coupling constants in C13 spectral editing techniques-INEPT, DEPT
methods.
2D NMR: Introduction, different types of 2D experiments- 2D-J resolved spectroscopy,
correlation spectroscopy (COSY), HOMO COSY and HETERO COSY (HETCOR).
Qualitative and quantitative applications of H1NMR: Proton NMR spectrum of paracetamol,
aspirin, salbutamol, benzocaine, phenacetin & clofibrate.Quantitative analysis of Aspirinparacetamol-codiene tablets
Ph.C-26: Mass spectrometry:
Origin of spectrum, principle and instrumentation of EI mass spectrometer, types of fragments,
odd electron containing neutral and charged species, Nitrogen rule, odd and even mass and odd
electron and even electron containing cations. Isotopic peaks, common mass fragmentation
patterns of organic compounds- Fragmentation of simple hydrocarbons, aromatic compounds,
alcohols, carbonyl compounds, carboxylic acids, esters & amides. McLafferty rearrangement,
Retro-Diels-Alder fission, ortho effect.
Ph.C-27: Advanced techniques & Applications of Mass spectrometry:
High resolution masss spectrometer and instrumentation, Limitations of EI technique, Ionization
techniques – Chemical Ionization, Fast Atom Bombardment (FAB), Secondary Ion mass
Spectrometry (SIMS), Thermospray , Electrospray, Matrix assisted laser desorption ionization,
Californium plasma desorption ionization. Mass analyzers – magnetic analyzer, electro
magnetical analyzer, quadrupole, time of flight and ion trap.
EI mass spectra of Limonene, bupivacaine (-cleavage), chloroquine, propranolol, famotidine,
butorphanol. .
Ph.C-28: Principles and pharmaceutical applications of AAS , AES and
Spectroflorimetry
Atomic absorption spectroscopy: Principle, instrumentation- radiation source, atomic vapour
producers, monochromator, detector, amplifier; detection limit and sensitivity. Interferences.
Analytical techniques- calibration curves, standard addition method. Applications: Assay of total
23
zinc in insulin zinc suspension, determination of thiomersal as mercury in a solution for contact
lenses.
Atomic emission spectroscopy(Flame photometry): Principle, instrumentation-burner, mirrors,
slits, monochromators, filters, detectors. Quantitative analysis- Direct caliberation, standard
addition method, internal standard method. Applications- Determination of calcium in
magnesium chloride for dialysis, determination of the concentration of potassium in
haemodalysis solution.
Spectrofluorimetry: Theory, instrumentation, fluorescence and structure, effect of structural
rigidity, temperature and solvent effects, effect of concentration on fluorescence intensity,
Quantitative aspects, applications- determination of proflavin hemisulphate in proflavin cream,
determination of ethinyloestradiol tablets
Recommended text books:
1. NMR in Chemistry-A multinuclear introduction. By William Kemp
2. Spectroscopic identification of Organic Compounds. By Silverstein, Basseler &
Morril
3. Spectroscopic identification of Organic Compounds. By P.S.Kalsi
4. Organic Spectroscopy. By William Kemp
5. NMR spectroscopy. By Grunther
6. Organic spectroscopy. By Fleming
7. Advances in NMR spectroscopy. By Saunders etal
8. Introduction to spectroscopy by Pavia
9. Pharmaceutical analysis by Watson
10. Practical pharmaceutical chemistry by Beckett & Stenlake
11. Mass spectroscopy by Dass
12. Mass spectrometry of organic compounds by Herbert Budzikiewicz, Carl Djerassi &
Dudley H.Williams
13. Mass spectrometry by Hoffmann
14. Mass spectrometry for chemists and biochemists by Johnstone
15. Analytical chemistry by Christian
16. Fundamentals of analytical chemistry by Skoog, West, Holler
24
PAPER –III(Ph.C –203):
BIOPHARMACEUTICALCHEMISTRY
AND PHARMACODYNAMICS
Ph.C-29:
Fermentation Technology
Ph.C-30
Enzymes and Biotransformations
Ph.C-31:
Drug Interactions
Ph.C-32:
Pharmacodynamics
Ph.C-29: Fermentation Technology
Introduction to Microbiology - staining methods .Sterilization and disinfection- physical
agents.(sunlight, heat, dry heat , moist heat filtration, radiation ultrasonic and sonic
vibrations).chemicals (alcohols, aldehydes, dyes, halogens, phenols, surface active agents,
metallic salts and gases).Culture media - basic requirements, types of media
Fermentation Technology- Introduction; development of industrial microroganisms-mutatoins,
selectiion of mutants, selection of secondary metabolite producing mutants, catalyst screening,
industrial fermentation (brief discussion only), maintainance of aseptic conditions, oxygen
transfer; applications; b-lactam antibiotics- penicillins, streptpmycin, tetracyclins,
chloramphenicol, vitamins- vit.B2, vit C, ergot alkaloids.
Ph.C-30: Enzymes and Biotransformations
Enzymes: Introduction; Classification and nomenclature of enzymes; mechanism of enzyme
action- lock and key model; induced fit model; enzyme kinetics-initial velocity, effect of enzyme
concentration substrate concentration (Michaels- Menton equation Lineweaver-Berk
representation), effect of pH, temp.; Enzyme inhibition- irreversible, reversible(competitive, noncompetitive and uncompetitive). Immobilization of enzymes- adsorption method, chemical
binding method, cross binding method, entrapping method, effect of immobilization on kinetics
and properties of enzyme applications and production of penicillin’s , steroids, L-DOPA
BiotransformationsIntroduction; biotransformations with special reference to steroids and
sterols- hydroxylation, dehydrogenation, hydrogenation, epoxidation, ring A aromatization,
synthetic routes. Biotransformations with reference to prostaglandins -synthhesis of PGE1
sulprostone, Anti tumour drugs – Hycanthone, Oxaminoqine
Ph.C-31: Drug Interactions
Introduction, classification – pharmacokinetic interactions(alteration of gastrointestinal
absorption, compexation and adsorption, alteration of distribution, alteration of metabolism and
alteration of excretion) & pharmacodynamic interactions (antagonistic effects, synergistic
effects, alteration of electrolyte levels, interactions involving adrenergic system, alteration of
receptor site interaction and antibiotic combinations). Mechanisms of drug interactions.
Influence of alcohol (antibiotics, anti coagulants, anti histamines, anti psychotic drugs , sedatives
& hypnatics), smoking (theophylline, diazepam & tricyclic anti depressants) and food
(bronchodilators, diuretics, ACE inhibitors, anti coagulants, tetracyclines) on drug action
Ph.C-32: Pharmacodynamics
Introduction, targets for drug action, receptor concept. Pharmacological binding terms. Twostatereceptor model, receptor families- structure and signal transduction mechanisms- channel
linked proteins, gating mechanism, G-protein coupled receptors, G-protein and their role, Targets
25
for G-proteins, Kinase linked receptors, receptors that regulate gene transcription. Theories of
concentration -response relationship, dose-response curves.
Recommended text books:
1. Text Book of Microbiology By Ananthanarayanan & Jayaram panikar
2. General principles of Microbiology By Stainer
3. Biochemistry. By Lehninger.
4. Biochemistry. By Stryer.
5. Biochemistry. By Rastogi.
6. Biochemistry. By Chatwal.
7. Biochemistry. By Well.
8. Pharmaceutical Biotechnology. By Kor and Hal Kari
9. An introduction to biotransformation in organic chemistry By JamesR.Hanson
10. Biotransformation by Faber
11. Pharmaceutical Biotechnology. By Kor and Hal Kari.
12. Biopharmaceutics and Pharmacokinetics by Brahmankar
13 Goodmann & Gilmann’s “ The pharmacological basis of therapeutics. By
Gilman & Rali.
14 Parmacology. By Rang.&Dale
References:
1. Pharmaceutical Biotechnology. By Vyas and Dixit.
2. Biotechnology. By John .E.Smith.
3. Genetic Engineering and it’s Applications. By Joshi.
4. Molecular Biotechnology. By Click etal.
5. Pharmaceutical Biotechnology. By Kor and Halkari.
6. Pharmaceutical Biotechnology. By Vyas and Dixit.
7. Medical Biotechnology By Jogdanand
8. Instant notes on Genetics By Winter, Hickey and Fletcher
9. Pharmaceutical Microbiology By Hugo and Russell
10 Remington ?
26
PAPER –IV (Ph.C- 204): NATURAL PHARMACEUTICALS
Ph.C-33: Herbal Drugs.
Ph.C-34: Alkaloids
Ph.C-35: Glycosides and Prostaglandins
Ph.C-36: Steroids and Hormones
Ph.C-33 Herbal Drugs.
i)Classification of herbal drugs- Taxonomical, Morphological, Pharmacological and Chemical
classification. ii) Adulteration and evaluation of drugs. iii) Different chemical groups of Herbal
drugs-- Alkaloids, Terpenoids, Glycosides.
Isolation and structure determination of terpenoids ,synthetic methods and analysis of natural
pharmaceuticals (colour reactions, chemical analysis).
Ph.C-34: Alkaloids
Introduction, Source, isolation, general methods of structure determination. Synthesis, structure
determination , pharmacological activity and analysis of - Atropine, Morphine, Reserpine and
Quinine.
Ph.C-35: Glycosides and Prostaglandins
Glycosides: Introduction, Source, isolation structure, biogenesis, pharmacological activity and
analysis of: Digitoxin, Digoxin, Sennosides, erythromycin and streptomycin .
Prostaglandins: Introduction, source, Isolation, classification, structure determination, synthesis,
pharmacological activity and analysis of: Prostaglandins E1, E2, E3, F1, F2. Structure of H and
thrombaxane.
Ph.C-36: Steroids And Hormones
Steroids : Introduction ,Source, Isolation, structure detremonation, synthesis , pharmacological
activity and analysis of : cholesterol, cholic acid.
Hormones: Introduction, source, Isolation, classification, structure determination , synthesis ,
pharmacological activity and analysis of : androsterone, progestrone and cortisone, thyroxine.
Recommended text books:
1. Natural products. By P.S.Kalsi
2. Organic natural products By Barton and Ollis
3. Alkaloids. By Manske
4. Alkaloids By Pelletier
5. Alkaloids By Bentely
6. Organic natural products by OP Agarwal
7. Natural products. By P.S.Kalsi
8. Organic natural products By Barton and Ollis
9. Organic Chemistry By IL Finar vol1,2
10. Medicinal natural products by Dewick
27
11.
12.
13.
14.
15.
16.
17.
The chemistry of terpenes by Pinder
Chemistry of steroids. By Fieser & Fieser.
Steroid chemistry. By Kalsi
Medicinal natural products by Dewick
Organic chemistry. By Finar. Vol.I & II
Prostaglandins. By Mitra.
Prostaglandins. By Ramsay
28
PAPER-V (Ph.C- 205):
Ph.C-37:
Ph.C-38:
Ph.C-39:
Ph.C-40:
CHIROTECHNOLOGY
Optical isomerism
Chirality & Biological activity
Conformational isomerism & biological effects
Asymmeteric Synthesis
Ph.C-37: Optical isomersm
Introduction to stereo isomerism. Definition and classification. Criteria for chirality.
Definitionm of molecular symmetry. Symmetry operations, symmetry elements (Cn,Ci & Sn).
Point group classification. Chiral point groups. Classification into dissymetric and asymmetric
molecules. Definition of enantiomers, diasteromers. Molecules with single chiral centre.
Molecules with 2 or more chiral centres. Examples with dissimilar and similar chiral centres.
Molecules with chiral axis. eg: Allenes, Spiranes and biphenyls. Configuration, Racemisation,
Racemic mixture - R,S configuration,Examples of chiral pharmaceuticals: DOPA, Thalidomide,
Ibuprofen, Salbutamol,.
Ph.C-38: Chirality and Biological activity
Influence of chirality on biological activity. Fischer’s lock and key concept, receptor theory ,
three point contact model.Definition of Eutomer and Distomer, Pfiffer’s rule. Eudesmic ratio.
Role of chirality on the biological activity of pharmaceuticals. Distomers - a) with no side effects
b) with undesirable side effects c) both isomers having independent therapeutic value d)
combination products having therapeutic advantages e) metabolic chirality inversion-eg:
Ibuprofen and related anti inflammatory drugs. Racemate resolution general methods i) via
crystallisation-eg: DL- threo Chloramphenicol. ii) Enricment of partially resolved enantiomers.
iii) By diastereomer crystallisation:eg-S,S-Etambutol. Fogassy parameters. Marckwald principle
and reciprocal resolution, mutual resolution.
Synthesis of chiral pharmaceuticals: Menthol, S-Naproxen, S-Ibuprofen( anti inflamatory), STimolol, oxazolidone, R-epichlorohydrin ( - blockers), Captopril, Enalapril, R- carnitine(ACE
inhhibitors),Diltiazam ( Calcium antagonist), D-phenyl Glycine, D-p-hydroxyphenyl glycine(
Intermediates of -lactam antibiotics), Indanavir sulphate (HIV -1-protease inhibitor).
Ph.C-39: Conformational Isomerism
Introduction to conformational isomerism. Concept of dynamic stereochemistry. Molecular
deformation and steric strain. Study of conformations of acyclics- ethane,propane, n-butane.
Population of conformers and torsional angles,conformations of haloalkanes, halohydrins and
glycols. Conformationa enantiomers and diastereomers.eg- butane 2,3-diol, ephedrine and - ephedrine. Study of conformations of cyclic molecules- cyclopropane, cyclobutane, cyclopentane
, cyclohexane ( mono, di-1,2-,1,3- & 1,4-), cycloheptane,cyclooctane, decalins and hydrindanes.
Conformational structures of Tropane, pseudotropane, decahydro quinoline, cholesterol,
morphine, menthol and neomenthol. Conformational flexibility and multiple modes of biological
effects of neurohormones.eg: Acetyl choline,epinephrine, histamine.
29
Ph.C-40: Asymmeteric Synthesis
Selectivity in synthesis: Definition and explanation of following with examples Substrate
selectivity, product selectivity. Substrate enantioselectivity and Diastereoselectivity, product
enantioselectivity and Diastereoselectivity.
Topocity in molecules: Homotopic, enantiotopic and diastereotopic units. Explanation each
based on substitution/addition and symmetric criteria with examples.
Prochirality: Nomenclature of prochiral Ligands and faces. Optical purity ee,de,method for
estimation
Stereo selective reactions of carbonyl compounds:
1,2-Asymmetric induction –(1) Nucleophilic addition to carbonyl group with examples of
addition of organometallic reagents and reduction with metal hydrides Cram’s rule and its
limitations. Felkin-Anh model,
(2) Enantio selective Aldol with chiral auxillary.
(3) -alkylation reactions of chiral enolates using chiral auxillary Example Evan’s
oxazolidinone,S-prolinol
(4)Reduction with chiral LiAlH4 (BINAL-H),chiral boron hydride (Alpineborane) CBS
Stereoselective reactions of alkenes .
Asymmetric Diels-Alder reaction, Sharpless & Asymmetric Hydro Boration with
IPCBH2&IPC2BH
Recommended text books:
1. Stereochemistry : conformation and mechanism by P.S.Kalsi
2. Stereochemistry of carbon compounds by Eliel
3. Stereochemistry of organic compounds by Eliel
4. The third dimension in organic chemistry by Bassindale
5. Stereochemistry by Hallas
6. Stereochemistry by Potapov
7. Stereochemistry through solved problems by Kalsi
8. Stereochemistry of organic compounds By Nasipuri
9. Chirotechnology by Sheldon
10. Guide book to Organic synhesis. By Mackie,Smith and Atkins
11. Organic synthesis. By Michael B.Smith
References:.
1. Asymmetric organic reactions. By Morrison and Moscher.
2. Asymmetric synthesis. By Nogradi.
3. Selectivity in organic synthesis. By Ward.
4. Stereochemistry of organic compounds. By Eliel.
5. Top Drugs: Top synthetic routes. By John Saunders.
6. Medicinal chemistry. By Ashtoshkar.
7. Biochemical approach to Medicinal chemistry. By Thomas Nogrady.
8. The organic chemistry of Drug synthesis. Vol 1-6 By Ledneicer etal.
30
B: Laboratory Courses
PAPER-VI(Ph.C-251):QUALITATIVE ANALYSIS OF ORGANIC COMPOUNDS
& PHARMACEUTICALS.
a) Identification of single functional group in organic compounds and pharmaceuticals by a
systematic qualitative analysis involving Physical data BP / MP, Ignition test, Solubility, Extra
elements – N,S & Halogens, Functional groups tests, Preparation of crystalline derivative and
determination of their m.p.s and reference to literature to identify the compounds.The list of
functional groups and compounds for identification: (a) Carbohydrates (b) Carboxylic Acid (c)
Phenols (d) 1o- Amines (e) 2o-Amines (f) 3o – Amines (g) Amides (h) Anilides (i) Aldehydes
(j) Ketones (k)Esters (l)Nitro comps (m)Hydrocarbons (n) Ethers
b) Colour reactions of the following pharmaceuticals: Aspirin, Isoniazid,Analgin, Paracetamol,
Ascorbic acid, Methylsalicylate,,Dichlorophen, cholesterol andquinine.
PAPER VII–(Ph.C- 252): PHARMACEUTICAL ANALYSIS-II
Assay of Ibuprofen in tablets Assay of pharmaceuticals (Redox titrations)
Assay of analgin in tablets by iodometry
Assay of ascorbic acid in raw material by iodometry
Assay of isoniazid in tablets by iodometry
Assay of ascorbic acid in tablets by cerimetry
Determination of hydrogen peroxide in medicament by Permanganometry
Complexometric titrations:
Assay of Calcium in Calciumgluconate
Assay Zinc in Bacitracin zinc
Non-aqueous titrations:
Assay of diphenylhydramine hydrochloride in tablets
Assay of ephedrine hydrochloride in capsules
PAPER –VIII(Ph.C- 253): INSTRUMENTAL ANALYSIS-II
Assay of Riboflavin in tablets by UV-Visible Spectrophotometry
Assay of Diazepam in tablets by UV-Visible Spectrophotometry
Assay of Nimuselide in nimuselide tablets by UV-Visible Spectrophotometry
Dissolution profile of paracetamol & ampicillin
Determination of sodium and potassium ions in pharmaceuticals by flamephotometry
Determination of quinine sulphate& Riboflavin by florimetry.
Potentiometric titration of strong acid vs strong base
Potentiometric estimation of Sulphanilamide and Atropine
Determination of moisture content in Paracetamol, Ascorbic acid and ampicillin by Karl-Fischer
method.
.
31
M.Sc Pharmaceutical Chemistry
III Semester Syllabus
A. Theory Course
PAPER-I (Ph.C- 301): CHEMISTRY OF PHARMACOLOGY
Ph.C-41:
Ph.C-42:
Ph.C-43:
Ph.C-44:
Classification of pharmaceuticals & drugs acting on nervous system:,
Cardiovascular agents and Hematological agents
Chemotherapeutics
Gastro intestinal agents, Diuretics,& Anti inflammatory agents.
Ph.C-41: Classification of pharmaceuticals & drugs acting on nervous system:
Definition of pharmaceuticals. Classification based on structure, disadvantages. Classification
based on therapeutic activity& target .Drugs acting on nervous system: Introduction to nervous
system, neurotransmission. Classification to Central nervous system drugs and peripheral
nervous system drugs. Pharmacology, mode of action and adverse effects of CNS depressants.
I) General anesthetics. eg.Haloethanes, Thiopental ii)Hypnotics and sedatives. eg.
Benzodiazepines and barbiturates. iii)Non- opioid analgesics. eg. Salicylates, p-amino phenol
derivatives, acetaminophen iv) Opioid analgesics: eg Morphine, codeine and meperidine
v)Antipyretics: eg. Aspirin, paracetamol vi)Anticonvulsants eg. benzodiazepine, strychnine and
LSD vii)Antipsychotic agents:eg. phenothiazines, butyrophenones viii) Antianxiety agents.
eg.Chlorezepam, alprazolam and diazepam ix)Antiparkinsons agents: eg.L-DOPA, carbidopa.
Pharmacology, mode of action and adverse effects of CNS stimulants. i)) Analeptics: eg.-- ii)
Antidepressents: eg. Tricyclics, Fluoxeline iii) Opiad analgesics: Morphine, Codeine, and
Methadone.Peripheral Nervous system drugs i)Adrenergic stimulants: eg.Epinephrine,
Amphetamine and Ephedrine ii) Local anesthetics: eg.Procaine and Veratridine iii)Antitussives:
eg.Noscapine, chlophdianol and benadryl. iv)Cholinergic agonists: eg. Acetylcholine, bethenecol
v)Anticholinergic agents:eg.Atropine, nicotine
Ph.C-42: Cardiovascular agents and Haematological agents
Introduction to cardiovascular system, structure of heart and cardiac out put, cardiac cycle.
Pharmacology, mode of action and adverse affects of :i)Cardiotonic drugs. eg: digitoxin, digoxin,
Agonists- dopamine, dobutamine. Vasodialators- Nitroprusside.
ii) Anti-arrhythmic:Class-I Quinidine ( Procanamide), Class-II eg: Lidocaine,Class-III:
Propranolol ,metaprolol, Class-IV Bretylium, Class-Veg: Verapramil iii) Antianginal drugs eg.
Organic nitrites- Nitroglycerine, Ca2+ blockers; Nifedepine, blockers- Propranolol
iv)Anti hypertensive drugs. eg: ACE inhibitors-eg: captopril, enalapril, Ca2+channel blockersNicardipine .Haemotological agents.Composition of blood, function, clotting, clotting factors,
terminology, formation of platelet aggregation- activating and inhibiting signals. Platelet
inhibitor drugs: aspirin dipyridamol, anticoagulants- blood coagulatin- extrinsic and intrinsic
pathways. Heparin and coumarols (warfarin and dicoumarol). Thrombolytic drugs. Introduction
eg. alteplase: streptikinase , urokinase.
32
Ph.C-43: Chemotherapeutics
Introduction to chemotherapy. Basic principles- Drug resistance, drug synergism, Antibacterial
agents : antifolates- mode of action of sulfonamides, diamino pyrimidines, sulfones.
Sulfonamides - structures of
sulfanilamide, sulfamethoxazole.
Diamino pyrimidinestrimethoprim, Sulfones-dapsone.Cell wall synthesis inhibitors: structures of naturally occurring
penicillins and cefalosporins. Structure of cell wall. Mode of action of beta lactam antibiotics.
Resistance to beta lactamase. Beta lactamase inhibitors. Clavulanic acid sulbacturm.
Semisynthetic penicillins- Structures of ampicillin and amoxycillin.
Semisynthetic
cefalosporins-Structures of cefalexin, cefaclor.
Structures and mode of action of: drugs acting on cell membrane- polymixins. Antitubercular
drugs- cycloserine, isoniazid,. Antifungal drugs-miconazole, flucytosine.Antiprotozoal drugsantimalarial drugs- chloroquin. Antiamoebic drugs-tinidazole, metronidazole. . Anti viral
drugs- AZT, acyclovir.anticancer drugs-, 5-flouro uracil. DNA alkylators-, cyclophosphamide.
Antibiotics- daunorubicin, doxorubicin,. Microtubule inhibitors-taxol .
Ph.C-44: Gastro intestinal agents, Diuretics, & Anti inflammatory agents.
Gastrointestinal agents: Introduction to anatomy and brief physiology of gastrointestinal system
and gastrointestinal disorders. Drugs which increase gastrointestinal motility-laxatives, motility
stimulants-eg.metaclopramide, Drugs which decrease gastrointestinal motility-Anti diarrhoeal
drugs (eg. loperamide), Anti spasmodic drugs (eg. propantheline, dicyclomene). Drugs used to
dissolve gallstones-chendeoxy cholic acid, ursodeoxy cholic acid. Inflammatory-Bowel diseasePrednisolone. Antiemetic drugs-cyclizine, scopolamine. drugs used to treat peptic ulcersAntacids, omeprazole.Diuretics: Brief introduction to anatomy & physiology of kidneys.
.Antiulcer agents cimetidine, ranitidine and omeprazole.
Introduction to diuretics, their therapeutic uses and mechanism of action of-Site 1 Diureticscarbonic anhydrase inhibitors -eg.Acetazolamide, Site 2 Diuretics- furosemide.Site 3 DiureticsThiazide & related agents - eg. Thiazides, chlorothiazide.Site 4 Diuretics-spironolactone..
Drugs used in treatment of Gout: Etiology, treatment eg.Colchicin, Allopurinol.
Autocoids & Autocoid Antagonists: Definition of Autocoids and autocoid antagonists,
therapeutic uses of i)Prostaglandins-Carboprost ii) Drugs used for migraine--blockers,
sumatriptan
Recommended text books:
1. Introduction to drug design. By Silvermann
2. Comprehensive medicinal chemistry. Vol 1-5 By Hanzsch.
3. Principles of medicinal chemistry. By William Foye
4. Biochemical approach to medicinal chemistry. By Thomas Nogrady.
5. Textbook of organic medicinal and pharmaceutical chemistry. By Delgrado and
William
6 Introduction to Medicinal chemistry. By Patrick.
References:
1. Introduction to medicinal chemistry. How drugs act and why. By Alex Gringauz.
2. Hand book of pharmaceuticals. By Shenoy and Shenoy.
3. Medicinal chemistry: an introduction. By Gareth Thomas.
4. Pharmacology. By Rang,Dale and Ritter.
5. Burger’s medicinal chemistry and drug discovery. By Manfred E. Wolf.
33
6. Modern pharmacology with clinical applications. By Charles. Craig and Robert.
E.Sitzel.
7. Pharmacology by Lippingcot
34
PAPER-II(Ph.C- 302): PHARMACOKINETICS AND THERAPEUTICS
Ph.C-45: Pharmacokinetics – I
Ph.C-46: Pharmacokinetics - II
Ph.C-47: Principles of Therapeutics
Ph.C-48: Drug delivery systems
Ph.C-45: Pharmacokinetics-I
.Introduction and importance of ADME studies of drugs. Routes of administration .
i)Absorption: Definition, absorption of drugs across the membranes. Physico chemical factors
affecting the drug absorption (emphasis on pH partition hypothesis). Methods of determination
of drug absorption. Bioavailability, factors affecting bioavailability. ii)Distribution: Apparent
volume of drug distribution. Factors affecting distribution, plasma protein binding. iii)
Metabolism: Sites of drug metabolism, metabolic rate constant, bioactivation and
biotransformation of drugs ( phase I and phase II reactions) iv)Elimination: Types of elimination
and overall apparent elimination rate constant and half-life, concept of clearance.
Ph.C-46: Pharmacokinetics-II
Compartmental models: one, two (i Intravenous bolous injection ii.Intravenous
infusion,iii.extravascular administration) and non-compartmental approaches to pharmaco
kinetics. Application of these models to determine the various pharmacokinetic parameters.
Calculations
Non-linear pharmaco kinetics: causes of nonlinearity , Michaels-Menten kinetics- characteristics
, basic kinetic parameters. Calculations.
Ph.C-47: Principles of Therapeutics
Definition and explanation of various terms: MEC, MSC, MTC, AUC(graph). Peak plasma
concentration, time of peak concentration. Therapeutic range. Steady state concentration, onset
of action, onset of time, duration of action, intensity of action. LD50, ED50. Therapeutic
objective.
Dosage regimen, Design of dosage regimes: Dose size, dosing frequency, drug accumulation
during multiple dosing, time to reach steady-state during multiple dosing, average concentration
and body content on multiple dosing to steady state, loading dose, maintenance dose,
maintenance of drug within the therapeutic range, design of dosage regimen from plama
concentration. Modification to dosage regime: Dosing of drugs in obese patients, dosing of drugs
in Neonates, infants & children, dosing of drugs in geriatrics (elderly), dosing of drugs in
Hepatic disease, dosing of drugs in renal disease. Drug level monitoring.
Ph.C-48 :Drug delivery systems:
Controlled release of drug delivery systems, design of controlled drug delivery systems,
pharmacokinetics principles in the design and fabrication of controlled drug delivery systems,
drug release patterns of controlled delivery dosage forms and oral controlled release systems ,
parenteral controlled release systems, transdermal drug delivery systems, ophthalmic drug
delivey systems, intravaginal and intrauterine drug delivey systems, Bioavailability testing of
controlled release formulations.
35
Recommended text books:
1. Pharacokinetics. By Shobha Rani
2. Elements of Pharmacology. By Gandhi,Desani & Goyal.
3. Goodmann & Gilmann’s “ The pharmacological basis of therapeutics. By Gilman &
Rali.
4. Pharmacology. By Rang.
5. Biopharmaceutics and pharmacokinetics By Brahmanikar
6. Pharmacology By Lippincot
7. Modern Pharmacology with Clinical Applications. By R.Craig.
8. Compehensive pharmacy review by Leon Shargel
9. Hospital and clinical pharmacy
36
PAPER-III (Ph.C- 303): ANALYSIS BY SEPARATION TECHNIQUES
Ph.C-49:
Ph.C-50:
Ph.C-51:
Ph.C-52:
Applications of solvent extraction and Principles of
Chromatography
Gas chromatography ,GC-MS and GC-FTIR
HPTLC, HPLC and HPLC-MS
SEC, CE, SCFC and UPLC
Ph.C-49 Applications of solvent extraction and Principles of Chromatography
Types of extraction procedures – batch extraction, continuous extraction, counter current
extraction. Super critical fluid extraction, Soxhelt extraction. Determination of salts of organic
acids and bases, detemination of alkaloids in crude drugs, use in assay of cyclizine lactate
injection, Vitamine A tablets, PGE1 .
Chromatography:Introduction, classification of chromatographic techniques, differential
migration rates - partition ratio, retention time, relation between partition ratio and retention
time, capacity factor,selectivity factor. Efficiency of separation – resolution, diffusion, plate
theory and rate theory.
Ph.C-50: Gas chromatography , GC-MS and GC-FTIR
Principle, Instrumentation, Supply of carrier gas, stationary phases,sample injection system,
column, detectors (TCD, FID, ECD, N/P & FPD), derivatisation techniques, programmed
temperature gas chromatography, chiral selectivity. Methods of quantitation, specific
applications- analysis of methyl testosterone in tablets, analysis of atropine in eye drops,
Residual solvents/ organic volatile impurities by Head space gas chromatography.
GC-MS: Principle, instrumentation, interfaces, jet separator, mass analyzer, mass chromatogram,
ionization techniques (electron impact, positive ion chemical ionization, negative ion chemical
ionization), application to impurity profiling (eg. Propranolol)
GC-FTIR: Principle, instrumentation
Ph.C-51: HPTLC, HPLC and HPLC-MS
HPTLC: Principle, Technique, advantages over TLC eg: Determination of Lamivudine
HPLC: Principle, types of HPLC, Instrumentation, stationary phases, mobile phases, pumps,
gradient formers, sample injection, columns, detectors (fixed wavelength UV detector, variable
wavelength UV detector, photodiode array detector, electrochemical detector, Refractive index
detector, fluorescence detector) Technique: Derivatization in HPLC. Separation of enantiomers
by chiral HPLC. Methods of quantitation. Specific applications- assay of paracetamol and
aspirin in tablets. Assay of hydrocortisone cream.
HPLC-MS: Instrumentation, principle, interfaces - direct liquid introduction, moving belt
interface, particle beam interface, thermospray, electrospray, atmospheric pressure chemical
ionization interface and applications : Impurity profile of famotidine.
Ph.C-52: SEC,CE,SCFC and UPLC
Size-exclusion chromatography :Principle, Instrumentation, stationary phases, retention
behaviour applications: determination of relative component composition. Determination of
molecular weight eg. corticotrophin and insulin.
37
Capillary electrophoresis:Electrophoresis, electro osmotic flow, integration in CE,
instrumentation, control of separation, applications: Separation of Atenolol and related
impurities, analysis of nonsteroidal anti inflammatory drugs.
Super Critical fluid Chromatography: Principle, super critical fluids, instrumentation, stationary
phases, mobile phases, and detectors
Ultra Performance Liquid Chromatography: Principle, Instrumentation
Recommended text books:
1. Practical pharmaceutical chemistry. By A.H.Backette, J.B.Stenlake.
2. Fundamentals of analytical chemistry. By Skoog and West.
3. Pharmaceutical analysis. By Takeru,Higuchi
4. Pharmaceutical analysis By. Whatson
5. Pharmaceutical analysis By Chapman
6. Pharmaceutical analysis By Ashtoshkar .
7. Instrumental methods of chemical analysis By Sharma
References:
1. Chemical HPTLC & applications By Sethi
2. Gas chromatography By Willett
3. High pressure liquid chromatography By Veronica and Meyer & Beene
4. Analytical chemistry By Harris
5. High performance liquid chromatography By Lindsay
6. Vogel’s quantitative analysis
38
PAPER-IV(Ph.C-304): PHARMACEUTICAL DESIGN AND DEVELOPMENT
Ph.C-53
Ph.C-54
Ph.C-55
Ph.C-56
Principles Of Drug Discovery & SAR studies
QSAR Studies
Molecular Modeling
Modelling Biomolecules
Ph.C-53: Principles Of Drug Discovery & SAR studies
Drug discovery without lead –Serendipity- Pencillins and Librium. Lead discovery- random
screening nonrandom screening.( screening of natural products, medical folklore, screening
synthetic banks).
SAR studies : Introduction i.Binding role of hydroxy group, Amino group, aromatic ring, double
bond, ketones and amides. ii. Variation of substituents- alkyl substituents, aromatic substituents,
extension of structure, chain extension/contraction, ring expansion/contraction, ring variation,
ring fusion.Isosteres.iii. Simplification of the structure, rigidification, conformational blockers,
X-ray crystallographic studies. Drug development based on SAR-Morphine modification
.Development of Cimetidine and Captropril from the lead molecules.
Clinical observations: phase I, phase-II, phase-III, phase -IV trials.( Introductory treatment).
Ph.C-54: QSAR Studies
Introduction. A) QSAR parameters – Substituent constants- i.Linear relationship between log p
and biological activity ii.Non-linear relationship between log p and biological activity.Electronic
parameters, Steric parameters, effect of electronic and steric parameters on lipophilicity.B.
Methods used in QSAR studies-i.Linear free energy relationship (LFER). Application of
Hammet equation, Hansch analysis, significance of slopes and intercepts in Hansch analysis.
ii.Craig’s plot. iii.Topliss scheme iv.Free Wilson model – advantages and disadvantages
v.Cluster significant analysis vi.Minimal topological difference method.QSAR case study – on
Pyranenamine. Achievements of QSAR – Forecasting biological activity, selection of proper
substituents, bioisosterism, drug receptor interactions and pharmacokinetic information.
Ph.C-55: Molecular Modeling
Introduction to Quantum, classical and statistical mechanical approaches to molecular modeling.
Property evaluation through approximate molecular orbital procedure. Brief introduction to
schrodinger wave equation, Born –Oppenheimerr approximation, Hartree approximation. Huckel
molecular orbital theory and the approximations in HMO. Illustration(using butadiene, allyl
cation, anion and radical) of calculating wave functions and electron density through Huckel
molecular orbital theory. Local and global minima. Potential energy surfaces, Co-ordinate
system(Cartesian and Polar) Geometry optimization procedures. Differences between Quantum
mechanical and classical mechanical approaches. Empirical force field
(Molecular
mechanics)methods. Potentioal for bond stretching, bending, torsional, columbic and non bonded
interactions. Quaitative (brief) exposure to molecular dynamics simulations, conformational
analysis.
39
Ph.C-56 : Modeling Biomolecules
Challenges and limitations of quantum chemical and molecular mechanics methods in modeling
biomolecules: Nucleic acids, proteins, carbohydrates and lipids. Protien folding. Protien structure
prediction, Ramachandran plot. Secondary structure. Comparative protein modeling. Homology
modeling, ab initio structure perdiction and threading.
Computer aided drug design. Structure and analog based approaches. Quantitative structure
activity relationships. Pharmacophore based approaches. Molecular docking. De novo ligand
design.
Recommended books:
1.
2.
3.
4.
5.
6.
7.
Burger’s medicinal chemistry and drug discovery. By Manfred E. Wolf.
Introduction to Medicinal chemistry. By Patrick.
Introduction to drug design. By Silverman
Comprehensive medicinal chemistry. Vol 1-5 By Hanzsch.
Principles of medicinal chemistry. By William Foye
Biochemical approach to medicinal chemistry. By Thomas Nogrady.
Pharmaceutical Chemistry and Drug synthesis By Roth and Kleeman
References:
1. Drug design By E.J. Arienes
2. Jenkin’s quantitative pharmaceutical chemistry By Knevel and Dryden
3. Recent advances in Bioinformatics By IA.Khan and A Khanum
4. Computational chemistry By GH. Grant and WG. Richards
5. Molecular modeling By Hans Dieter Holtje and Gerd Folkers
6. Molecular modeling By Leach
7. Computational Chemistry by Jenson
40
PAPER-V(ID-Ph.Chem 305): CBCS
ID-1:
ID -2:
ID-3:
ID-4:
41
================================================================
B.Laboratory work
PAPER VI–(Ph.C-351):QUALITATIVE ANALYSIS OF ORGANIC MIXTURES &
QSAR STUDIES OF KNOWN BIOLOGIALLY ACTIVE SERIES
Seperation and analysis of organic binary and ternary mixtures.
QASR studies :
Generating the molecule using relevant modeling software and minimizing the energy
Obtaining the physico chemical parameters like Qlogp, , SMR using the software
Fitting the data to regression software (SPSS-10) and generating a models in which correlate
activity to its structure Projection of the best pharmacophore
PAPER-VII(Ph.C- 352): SYNTHESIS OF ORGANIC PHARMACEUTICALS
& ISOLATION OF HERBAL DRUGS.
Synthesis of : Benzocaine ( Anaesthetic), Antipyrine( Antipyretic),
Sulphonamide(antibacterial),Clofibrate( ), 2-phenyl indole , Quinoxalinone, Isoniazid(Anti
Tubercular ), Benzylic acid rearrangement, Beckmann rearrangement and stereoselective
reduction of ethyl acetoacetate by bakers yeast.
Isolation of Herbal Drugs:
1.Piperine from black Pepper 2. Caffeine from tea leaves 3. Menthol from mint leaves
4. Cineole from Eucalyptus leaves 5. Casein from milk.
PAPER-VIII(Ph.C- 353):
CHROMATOGRAPHY & SPECTRAL ANALYSIS OF
PHARMACEUTICALS AND INTERMEDIATES:
Thinlayer chromatography- Testing of purity , separation of mixtures and calculation of Rf
values.
Paper chromatography- Separation and identification of amino acids and chlorophylls.
Column chromatography- Separation and identification of chlorophylls, xanthophylls and
carotenes in leaves.
Ion-Exchange chromatography: Separation and estimation of metal ions ininorganic
pharmaceuticals.
High performance liquid chromatography- Determination of aspirin, paracetamol and caffeine in
APC tablets. 2. Determination of benzocaine and phenazone in eardrops. Identification of
unknown pharmaceuticals and intermediates by interpretation of IR,UV, Proton and C13 NMR
and Mass spectra
.
42
M.Sc Pharmaceutical Chemistry
IV-SEMESTER SYLLABUS
A. Theory course
PAPER-I (ID-Ph.Chem 401): CBCS
ID-1:
ID -2:
ID-3:
ID-4:
===============================================================
B.Laboratory work
Paper-II(Ph.C- 451): QUANTITATIVE ANALYSIS PHARMACEUTICALS:
Quantitative analysis- Estimation of 1. Assay of Amoxicillin2.Assay of Ethambutol 3.Assay of
adrenalin 4.Assay of Atropine in a mixture 5.Assay of Sulphanilamide.6. Assay of Amlodipine
7.Assay of Phenytoin 8.Assay of Phenacetin.
Paper-III(Ph.C- 452)
PROJECT / DESSERTATION WORK
1. Pharmaceutical synthesis
2. Pharmaceutical analysis (Physical,
chromatographic and biological methods).
chemical,
------------------------
electrochemical,
thermal,
spectral,
43
INTERDISCIPLINARY PAPERS (Choice based)OFFERED BY PHARMACEUTICAL
CHEMISTRY SECTION OF CHEMISTRY DEPARTMENT ,OU COLLEGE FOR
WOMEN.
ID/Ph.C/Pool-3
PAPER- Offered at III semester:
BIOPHARMACEUTICAL CHEMISTRY AND PHARMACO DYNAMICS
Unit-1:
Unit-2:
Unit-3:
Unit-4:
Fermentation Technology
Enzymes and Biotransformations
Drug Interactions
Pharmacodynamics
PAPER- Offered at IV semester:
NATURAL PHARMACEUTICALS
Unit-1:
Unit-2:
Unit-3:
Unit-4:
Herbal Drugs
Alkaloids
Glycosides and Prostaglandins
Steroids and Hormones
44
ID/Ph.C/Pool-3
PAPER- Offered at III semester:
BIOPHARMACEUTICALCHEMISTRY AND PHARMACODYNAMICS
Unit-1:
Unit-2:
Unit-3:
Unit-4:
Fermentation Technology
Enzymes and Biotransformations
Drug Interactions
Pharmacodynamics
Unit-1:
Fermentation Technology
Introduction to Microbiology - staining methods .Sterilization and disinfection- physical
agents.(sunlight, heat, dry heat , moist heat filtration, radiation ultrasonic and sonic
vibrations).chemicals (alcohols, aldehydes, dyes, halogens, phenols, surface active agents,
metallic salts and gases).Culture media - basic requirements, types of media
Fermentation Technology- Introduction; development of industrial microroganisms-mutatoins,
selectiion of mutants, selection of secondary metabolite producing mutants, catalyst screening,
industrial fermentation (brief discussion only), maintainance of aseptic conditions, oxygen
transfer; applications; b-lactam antibiotics- penicillins, streptpmycin, tetracyclins,
chloramphenicol, vitamins- vit.B2, vit C, ergot alkaloids.
Unit-2: Enzymes and Biotransformations
Enzymes: Introduction; Classification and nomenclature of enzymes; mechanism of enzyme
action- lock and key model; induced fit model; enzyme kinetics-initial velocity, effect of enzyme
concentration substrate concentration (Michaels- Menton equation Lineweaver-Berk
representation), effect of pH, temp.; Enzyme inhibition- irreversible, reversible(competitive, noncompetitive and uncompetitive). Immobilization of enzymes- adsorption method, chemical
binding method, cross binding method, entrapping method, effect of immobilization on kinetics
and properties of enzyme applications and production of penicillin’s , steroids, L-DOPA
BiotransformationsIntroduction; biotransformations with special reference to steroids and
sterols- hydroxylation, dehydrogenation, hydrogenation, epoxidation, ring A aromatization,
synthetic routes. Biotransformations with reference to prostaglandins -synthhesis of PGE1
sulprostone, Anti tumour drugs – Hycanthone, Oxaminoqine
Unit-3: Drug Interactions
Introduction, classification – pharmacokinetic interactions(alteration of gastrointestinal
absorption, compexation and adsorption, alteration of distribution, alteration of metabolism and
alteration of excretion) & pharmacodynamic interactions (antagonistic effects, synergistic
effects, alteration of electrolyte levels, interactions involving adrenergic system, alteration of
receptor site interaction and antibiotic combinations). Mechanisms of drug interactions.
Influence of alcohol (antibiotics, anti coagulants, anti histamines, anti psychotic drugs , sedatives
& hypnatics), smoking (theophylline, diazepam & tricyclic anti depressants) and food
(bronchodilators, diuretics, ACE inhibitors, anti coagulants, tetracyclines) on drug action
45
Unit-4: Pharmacodynamics
Introduction, targets for drug action, receptor concept. Pharmacological binding terms. Twostatereceptor model, receptor families- structure and signal transduction mechanisms- channel
linked proteins, gating mechanism, G-protein coupled receptors, G-protein and their role, Targets
for G-proteins, Kinase linked receptors, receptors that regulate gene transcription. Theories of
concentration -response relationship, dose-response curves.
Recommended text books:
1. Text Book of Microbiology By Ananthanarayanan & Jayaram panikar
2. General principles of Microbiology By Stainer
3. Biochemistry. By Lehninger.
4. Biochemistry. By Stryer.
5. Biochemistry. By Rastogi.
6. Biochemistry. By Chatwal.
7. Biochemistry. By Well.
8. Pharmaceutical Biotechnology. By Kor and Hal Kari
9. An introduction to biotransformation in organic chemistry By JamesR.Hanson
10. Biotransformation by Faber
11. Pharmaceutical Biotechnology. By Kor and Hal Kari.
12. Biopharmaceutics and Pharmacokinetics by Brahmankar
13 Goodmann & Gilmann’s “ The pharmacological basis of therapeutics. By
Gilman & Rali.
14 Parmacology. By Rang.&Dale
46
ID/Ph.C/Pool-3
PAPER- Offered at IV semester:
NATURAL PHARMACEUTICALS
Unit-1:
Unit-2:
Unit-3:
Unit-4:
Herbal Drugs
Alkaloids
Glycosides and Prostaglandins
Steroids and Hormones
Unit-1: Herbal Drugs.
i)Classification of herbal drugs- Taxonomical, Morphological, Pharmacological and Chemical
classification. ii) Adulteration and evaluation of drugs. iii) Different chemical groups of Herbal
drugs-- Alkaloids, Terpenoids, Glycosides.
Isolation and structure determination of terpenoids ,synthetic methods and analysis of natural
pharmaceuticals (colour reactions, chemical analysis).
Unit-2: Alkaloids
Introduction, Source, isolation, general methods of structure determination. Synthesis, structure
determination , pharmacological activity and analysis of - Atropine, Morphine, Reserpine and
Quinine.
Unit-3: Glycosides and Prostaglandins
Glycosides: Introduction, Source, isolation structure, biogenesis, pharmacological activity and
analysis of: Digitoxin, Digoxin, Sennosides, erythromycin and streptomycin .
Prostaglandins: Introduction, source, Isolation, classification, structure determination, synthesis,
pharmacological activity and analysis of: Prostaglandins E1, E2, E3, F1, F2. Structure of H and
thrombaxane.
Unit-4: Steroids And Hormones
Steroids : Introduction ,Source, Isolation, structure detremonation, synthesis , pharmacological
activity and analysis of : cholesterol, cholic acid.
Hormones: Introduction, source, Isolation, classification, structure determination , synthesis ,
pharmacological activity and analysis of : androsterone, progestrone and cortisone, thyroxine.
Recommended text books:
1. Natural products. By P.S.Kalsi
2. Organic natural products By Barton and Ollis
3. Alkaloids. By Manske
4. Alkaloids By Pelletier
5. Alkaloids By Bentely
6. Organic natural products by OP Agarwal
7. Natural products. By P.S.Kalsi
8. Organic natural products By Barton and Ollis
47
9. Organic Chemistry By IL Finar vol1,2
10. Medicinal natural products by Dewick
11. The chemistry of terpenes by Pinder
12. Chemistry of steroids. By Fieser & Fieser.
13. Steroid chemistry. By Kalsi
14. Medicinal natural products by Dewick
15. Organic chemistry. By Finar. Vol.I & II
16. Prostaglandins. By Mitra.
17. Prostaglandins. By Ramsay