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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