Download M.Sc.(PHARMACEUTICAL CHEMISTRY) PART

SYLLABUS
M.Sc. PHARMACEUTICAL CHEMISTRY PART-II
Examinations for 2015-16 & 2016-17 sessions
OUTLINES OF THE TEST
1.
The examination will consist of two semesters i.e. semester III and IV
2.
Each semester shall be of maximum 600 marks.
3.
Each theory paper shall be of 100 marks of which 70 marks shall be allocated to the theory
papers set by external examiner. The internal assessment in each paper shall be of 30 marks i.e.
Assignments /seminar of 12 marks, internal test of 12 marks (average of two shall be taken)
and 6 marks for attendance.
SEMESTER-III (November/December)
Paper
Theory IX
X
XI
XII
Practical V
VI
Title of paper
Marks
Medicinal Chemistry –I
New Drug Development & Toxicology
Pharmaceutical Technology-I
Drug Design and Drug Development – I
Analysis of Pharmaceuticals
Formulation of dosage forms
Total
100
100
100
100
100
100
600
SEMESTER-IV (April/May)
Paper
Theory XIII
XIV
XV
Practical-VII
Title of paper
Marks
Medicinal Chemistry-II
Drug Design & Drug Development-II
Pharmaceutical Technology-II
Synthetic Medicinal Chemistry
Project work
Total
100
100
100
100
200
600
M.Sc PHARMACEUTICAL CHEMISTRY
(SEMESTER-III)
PAPER-IX: MEDICINAL CHEMISTRY –I
Maximum Mark : 100
i)Theory Paper : 70
ii)Internal Assessment : 30
Time: 3 hours
Pass Marks : 35%
Lectures to be delivered : 60
INSTRUCTIONS FOR THE PAPER SETTERS:
The question paper will consist of three sections A, B and C. Section A and B will have four questions
from the respective sections of the syllabus and will carry 07 marks each. Section C will consist of a short
answer / objective type questions, which will cover the entire syllabus uniformly and will carry 28 marks (2
marks each).
INSTRUCTIONS FOR THE CANDIDATES:
1.
Candidates are required to attempt three questions each from sections A and B of the question
paper and the entire section C.
2.
The use of scientific calculators is allowed.
SECTION-A
i.
Introduction to Pharmaceuticals, Historical development, Classification of drugs,
Nomenclature of Pharmaceuticals & Drug metabolism reactions.
ii.
Structure, stereochemistry, nomenclature, mode of action, specific clinical
applications and structure activity relationships, biosynthesis of naturally occurring
compounds and synthesis of prototypical drugs in each category (Chemical &
Pharmacological) for the following classes of drugs.
Hormones: Sex hormones and related compounds (Estrogens, Androgens,
Progestational agents, Anabolic steroids, Contraceptives), Adrenal cortex
hormones, Thyroid hormones and antithyroid drugs, pancreatic hormones,
Hypothalamus hormones.
Vitamins: Fat soluble vitamins (A, D, E and K) , water soluble vitamins (Folic
acid, B12 and C).
Adrenergic and cholinergic drugs(Agonist & antagonists):
Sympathomimetics, Catecholamines, Phenylethamolamines, Phenylethlamines,
Non-catecholamines, Imidazoline derivatives, Adrenergic blocking agents.
Cholinergic agents: Autonomic blocking and related drugs. Antispasmodic and
antiulcer drugs. Antiparkinsonism drugs.
Structure, stereochemistry, nomenclature, mode of action, specific clinical applications and
structure activity relationships, biosynthesis of naturally occurring compounds and synthesis of
prototypical drugs in each category (Chemical & Pharmacological) for the following classes of
drugs.
Cardiovascular drugs:Vasodilators, Antihypertensive agents, Antihypercholesterolemic drugs,
Antiarrhythmic drugs, Sclerosing agents, Coagulants and anticoagulants, Cardiotonic
compounds,Cardiac glycosider & inotropic agents Synthetic hypoglycemic agents.
Diuretics: Osmotic agents, Acidfying salts, Mercurials, Purines and related heterocycles,
Sulfonamides, Benzothiadiazene and related compounds, Chlorothiazides and analogs.
Sulfamoylebenzoic acid and analogs, Endocrine Antagonists, Miscellaneous diuretics.
SECTION-B
Structure, stereochemistry, nomenclature, mode of action, specific clinical applications
and structure activity relationships, biosynthesis of naturally occurring compounds and synthesis
of prototypical drugs in each category (Chemical & Pharmacological) for the following classes
of drugs.
General Anesthetics: Theories of General Anesthetics, Ethers, Halogenated hydrocarbons,
Cyclopropane, Nitrous oxide, Barbiturates, Adjuncts to general anesthetics, metabolism of
volatile anesthetics.
Local anesthetics: Cocoa alkaloids – Cocaine and Synthetic compounds, Esters, Amides,
Miscellaneous anesthetics.
CNS Active Drugs: CNS Depressants: Hypnotics and sedatives: Barbiturates, Non barbiturates,
Amides and Imides, Bezodiazepines, Aldehydes and derivatives, Methaqualone and other
miscellaneous agents. Anticonvulsants: Barbiturates, Hydanatoins. Oxazolidinediones.
Succinmides, Bezodiazepines, Thenacemide, Glutethimide.
CNS-stimulants & Psychoactive drugs: Analeptics, Purines, Psyschomotor stimulants,
Sympathomimetics, Monamine oxidase Inhibitors. Tricyclic antidepressants, Miscellaneous
psychomotor stimulants.Hallucinogens (Psychodelics, Psychomimetics):Indolethylamines,
ß-phenylethylamines, Butyrophenones and other miscellaneous drugs.
Structure, stereochemistry, nomenclature, mode of action, specific clinical applications
and structure activity relationships, biosynthesis of naturally occurring compounds and synthesis
of prototypical drugs in each category (Chemical & Pharmacological) for the following classes
of drugs.
Analgesics and Antitussives: Morphine and related opioids, Narcotic antagonists, Synthetic
analgesics- Antitussives: Opium alkaloid, Morphine analogs, Synthetic non-narcotic antitussives,
mucolytic agents.
Antipyretics and Non-steroidal Anti-inflammatory agents: Salicyclic acid derivatives. Indolyl
and Arylacetic acid derivatives. Pyrazole derivatives. Aminophenol derivatives, Arylpropionic
acid derivatives, Salol Principle, Anti- Gout Drugs.
Antiallergics: Serotonin, Bradykinin, Antihistamines (ethylenediamine derivatives of aminoalkyl
ethers, derivatives of cyclic basic chains, Monoaminopropyl derivatives , Derivatives of tricyclic
compounds).
Radio Pharmaceuticals: Pharmaceutical examples for therapeutic & diagnostic agents
Precautions & safety measures for handling & disposing.
Books Recommended:
1.
Wilson and Gisvolds Textbook of Organic Medicinal and Pharmaceuticals
Chemistry, 8th edition, edited by R.F. Doerge, J.B. Lippincott Company,
Philadelphia, 1982.
2.
Pharmaceutical Chemicals in Perspective, B.G. Reuben and H.A. Wittcoff, John
Wiley & Sons, New York, 1989.
3.
W.C. Foye, Principles of Medicinal Chemistry, Lea & Febiger, Philadelphia,
U.S.A.
Suggested Readings:
Strategies for Organic Drug Synthesis and Design, D.Lendnicer, John Wiley and Son, New York,
1998.
M.Sc PHARMACEUTICAL CHEMISTRY
(SEMESTER-III)
PAPER-X: NEW DRUG DEVELOPMENT AND TOXICOLOGY
Maximum Mark : 100
i)Theory Paper : 70
ii)Internal Assessment : 30
Time: 3 hours
Pass Marks : 35%
Lectures to be delivered : 60
INSTRUCTIONS FOR THE PAPER SETTERS:
The question paper will consist of three sections A, B and C. Section A and B will have four questions
from the respective sections of the syllabus and will carry 07 marks each. Section C will consist of a short
answer / objective type questions, which will cover the entire syllabus uniformly and will carry 28 marks (2
marks each).
INSTRUCTIONS FOR THE CANDIDATES:
1.
Candidates are required to attempt three questions each from sections A and B of the question
paper and the entire section C.
2.
The use of scientific calculators is allowed.
SECTION-A
Common laboratory animals in pharmacology research, regulations for the care and use of
laboratory animals.
Preclinical safety evaluation of new chemical agent : Concept of LD50, Determination of LD50,
acute, sub-chronic and chronic toxicity studies.
Clinical evaluation of new chemical entity : Placebo, clinical trial study designs, phase of clinical
trials.
Bio assays: Basic principles of bio-assays, types of bioassays and application.
- RIA : Principles of RIA and application.
- ELISA : Principles and application.
SECTION-B
Toxicology : General principles of management of poisoning. Diagnosis and Management of
toxicity due to atropine, barbiturates , Morphine & Alcohol.
Experimental models to screen the following classes of drugs:-Analgesics
- Anti-inflammatory agents.
- Anti- psychotics
- Anti- depressants
- Anti-anxiety agents
- Anti-ulcer drugs
- Anti-diabetics
BOOKS RECOMMENDED
1.
F.C.Lu, Basic Toxicology : Fundamentals, Target Organs and Risk Assessment , 3rd
2.
3.
4.
edition, Taylor and Francis, Washington, U.S.A. 1996.
D.R. Laurence and A.L. Bachrach, (eds.) Evaluation of Drug activities
Pharmnacometrics Vol. I, Academic Press, London, U.K. 1964.
M.N. Ghosh, Fundamentals of Experimental Pharmacology, 2nd edition , Scientific
Book Agency, Calcutta, India, 1984.
H.G. Vogel and W.H. Vogel (eds.) , Drug Discovery and EvaluationPharmacological Assays, Springer Verlag, Berlin, Germany,1997.
M.Sc PHARMACEUTICAL CHEMISTRY
(SEMESTER-III)
PAPER-XI: PHARMACEUTICAL TECHNOLOGY-I
Maximum Mark : 100
i)Theory Paper : 70
ii)Internal Assessment : 30
Time: 3 hours
Pass Marks : 35%
Lectures to be delivered : 60
INSTRUCTIONS FOR THE PAPER SETTERS:
The question paper will consist of three sections A, B and C. Section A and B will have four questions
from the respective sections of the syllabus and will carry 07 marks each. Section C will consist of a short
answer / objective type questions, which will cover the entire syllabus uniformly and will carry 28 marks (2
marks each).
INSTRUCTIONS FOR THE CANDIDATES:
1.
Candidates are required to attempt three questions each from sections A and B of the question
paper and the entire section C.
2.
The use of scientific calculators is allowed.
i.
ii.
SECTION-A
Introduction to different Pharmaceutical dosage forms, with their advantages &
limitations, organoleptic additives and stabilizing agents (dyes, lakes, flavours,
suspending agents, emulsifying agents, anti oxidants, preservatives etc) used in
pharmaceutical dosage forms.
Preformulation considerations: Need for preformulation studies, methods used
for assessing drug-excipient interactions, Importance of physico-chemical properties
of drug in dosage form development (pH, pKa, partition coefficient etc).
Processing of tablets: Advantages and disadvantages of tablets, types of tablets. Granulation- dry,
wet and direct compression. Basic characteristics and properties of excipients used in different
types of granulation processes. Various additives used in tablet formulations.
Compression of tablet- compressing machines and their tooling, processing problems and their
remedy. Evaluation of tablets as per official standards.
Tablet coating: Coating principles and equipment, Coating processes-sugar coating, Film coating
and enteric coating. Materials used in coating. Film characteristics,defects and their remedies.
Evaluation of coated tablets.
SECTION-B
Processing of Capsules: Hard gelatin capsules- Materials and production . Filling equipment,
hand filling, semiautomatic and automatic filling. Operations, formulation. Finishing and
evaluation.
Soft gelatin capsule-manufacture process, nature of capsule shell and contents. Evaluation,
physical stability and packing.
Microencapsulation: Importance and applications of microencapsulation in Pharmacy. Various
techniques and equipment employed for microencapsulation.
Liquid dosage forms: Types, advantages and disadvantages.
a.
Monophasic liquid dosage forms: Techniques of increasing solubility of
drugs, other problems involved in preparation and stability of liquids.
b.
Biphasic liquid dosage forms:
i.
Suspensions: Preparation and evaluation of suspensions, stability testing.
Problems in suspension formulation, flocculated and non-flocculated
suspensions.
ii.
Emulsions: Advantages of emulsion dosage form, types, identification,
selection of emulsifying agents. Preparation, Calculation of HLB value
and stability studies.
Semi- Solid dosage forms: Types of semi-solid dosage forms ointments, creams
and suppositories. Bases used in their preparation and their characteristics. Brief discussion on
their evaluation.
Books Recommended:
1.
C.W. Copper and G. Gunn, Dispensing Pharmacy, CBS Publishers &
Distributors, Delhi-110032.
2.
L.Lachman et. al., Theory and Practice of Industrial Pharmacy, Varghese
Publishing House, Dadar, Bombay-400014,1987.
Suggested Readingss:
1. A.Osol Remington’s Pharmaceutical Sciences, XVIII edition, Mack Publishing co.,
Pennsylvania, USA, 1990.
2. The Pharmacopoeia of India. IIIrd Edition, Vol. I and Vol. II, 1996, Govt. of
India, Ministry of Health and Family Welfare Delhi.
3. British Pharmacopoeia, International Edition, 1993.
4. The United States Pharmacopoeia, XXII & NF XVII and addenda, 1995.
5. The Pharmaceutical Codex, 12th Edition, The Pharmaceutical Press, London,1994.
6. Patrick B. Deasy , Microencapsulation and related drug processes, Dekker series Vol.20.
7. F.J.R. Nixon, Microencapsulation, Dekker series Vol 3.
8. Joseph R. Robinson, Sustained and Controlled Drug Delivery Systems, Dekker Series. Vol. 6.
M.Sc PHARMACEUTICAL CHEMISTRY
(SEMESTER-III)
PAPER-XII: DRUG DESIGN AND DRUG DEVELOPMENT-I
Maximum Mark : 100
i)Theory Paper : 70
ii)Internal Assessment : 30
Time: 3 hours
Pass Marks : 35%
Lectures to be delivered : 60
INSTRUCTIONS FOR THE PAPER SETTERS:
The question paper will consist of three sections A, B and C. Section A and B will have four questions
from the respective sections of the syllabus and will carry 07 marks each. Section C will consist of a short
answer / objective type questions, which will cover the entire syllabus uniformly and will carry 28 marks (2
marks each).
INSTRUCTIONS FOR THE CANDIDATES:
1.
Candidates are required to attempt three questions each from sections A and B of the question
paper and the entire section C.
2.
The use of scientific calculators is allowed.
SECTION-A
Introduction to Drug Design & Drug Development : Definition, History (Chronological
Evolution), Drug design approaches, Lead optimization, de Novo drug design.
Quantum Mechanics: Introduction to quantum mechanics, postulates of quantum mechanics,
Schrodinger equation , Perturbation theories of drug action, Pullman’s dipositive bond theory ,
Role of charge transfer process in drug action, conformational aspects & molecular orbital
calculations , molecular orbital approach to drug design with examples.
Drug Receptor Interactions: Historical background, Receptor theories, Forces involved in drug
receptor interactions; covalent & non-covalent interactions ; Agonist &
antagonists.
QSAR Analysis : Parameters & Biological data for QSAR, Design of Test series in QSAR: Craig
plot, Topliss
operational scheme, cluster analysis. Quantitative models: Hansch
(Extrathermodynamic) , Free Wilson (Additivity model) , Mixed approach.
Statistical method for QSAR: Regression analysis, multiple regression, stepwise multiple
regression, Partial least square analysis. Validation of QSAR models.
SECTION-B
Pharmacokinetics in Drug designing: Pharmacokinetics, Environmental pharmacokinetics.
Single and two compartment pharmacokinetics. Pharmacokinetics of drug metabolism. Dissection
of a drug molecule in to biofunctional moieties. Modulation of pharmacokinetics by molecular
manipulations, Modulation of distribution of pharmacea over various compartments, Modulation
of time-concentration relationship . Lipinski Rule, QSPR, Biopharmaceutics. Generic equivalence
and non-equivalence. Role of biopharmaceutics in Drug designing.
Peptidomimetics: Peptidomimetics research, Rational design of Peptidomimetics, nonpeptide,
Ligands for peptide receptors, Applications of oligonucleotides in antiviral and antitumoral
chemotherapy. Antisense nucleotides designing. Carbohydrate based Therapeutics.
Prodrug Approach: Basic concept, Common promoities. Reversal of prodrugs- chemical and
enzymatic . Application of prodrug approach to alter taste and odour, reduction of pain at injection
site, reduction of gastrointestinal irritability. Alteration of drug solubility, increasing chemical
stability. Prevention of presystematic metabolism. Prolongation of drug action, Site spectic drug
delivery. Reduction in drug toxicity. Alteration of drug metabolism.
Books Recommended:
1.
2.
3.
4.
The Organic Chemistry of Drug Design and Drug Action. by R.B. Silverman,
Academic Press,1992.
Drug Designs- A series of monographs in medicinal chemistry edited by A.J.
Ariens. Ist edition. Vol. I, II, V, VIII & IX (only relevant chapters).
Comprehensive medicinal chemistry. Peragmon Press. 1990, Vol.4.
Burger’s Medicinal Chemistry & Drug Discovery . fifth edition vol-.I, Willey
Interscience.
Suggested Readingss:
1.
Medicinal Chemistry for 21st century edited by C.G. Wermuth, Blackwell
Scientific Publications, 1997.
M. Sc. PHARMACEUTICAL CHEMISTRY
(SEMESTER-III)
Practical Paper- V: Analysis of Pharmaceutical
Time: 4 hours
M. marks: 100
Total practical hours: 60
Suggested Experiments
1. Separation of components of APC by TLC.1HNMR & IR analysis of its components.
2. Qualitative applications of ultra-violet spectroscopy.
3. Quantitative application of infrared spectroscopy.
4. Determination of molecular weight by .1HNMR
5. Structural isomer identification by.1HNMR.
6. Analysis of benzene traces in alcohol, homologous benzene derivatives and amino acids by high
order derivatives UV spectroscopy.
7. Determination of water content by moisture balance and by Karl Fischer method.
8. Measurement of Specific Optical Rotation of ibuprofen and determination of unknown
concentration.
9. Volumetric analysis of ibuprofen in tablets.
10. Analysis of ascorbic acid in given tablets.
11. Spectrophotometric determination of aspirin content in soluble aspirin tablets.
12. Spectrophotometric determination of Paracetamol in tablets.
13.
14.
15.
16.
17.
18.
19.
20.
21.
22.
23.
Extraction of oxyphenyl butazone from tablets. Its spectrophotometric analysis.
Analysis of Ampicillin trihydrate.
Analysis of Dextrose.
Extraction of cholesterol from Gall Stones and its analysis.
Analysis of citric acid.
Determination of Vitamin B1 in given tablets.
Determination of vitamin B2 in given tablets.
Determination of ephedrine hydrochloride in given syrup.
Determination of tetracycline in given capsules.
Determination of phenobarbitone in given cough syrup
Determination of chloremphenicol in given capsules
To perform I.P. monograph of tablets.
To perform I.P. monograph of hard gelatin capsules.
Evaluation of injections (ampoules 2 ml. and 5 ml.)
In – vitro comparative study of the release and penetration of drugs from topical preparations.
Evaluation of sustained release oral formulation (s).
To study the dissolution rate of nitrofurantion /aspirin tablets.
Determination of activity of enzyme penicillin.
Analysis of activated charcoal.
To perform quality control tests on surgical gauge Bandage cotton.
Note: Any other experiment (s) may be included in support of the theoretical aspects of the course.
24.
25.
26.
27.
28.
29.
30.
31.
32.
M. Sc. PHARMACEUTICAL CHEMISTRY
(SEMESTER-III)
Practical Paper- VI : Formulation of dosage forms
Time: 4 hours
M. marks: 100
Total practical hours: 60
Suggested Experiments
1. Preparation of effervescent granules.
2. Preparation of cough syrup.
3. Formulation of tablet of Paracetamol.
4. Formulation of tablet of sodium bicarbonate.
5. Preparation of capsule each containing 250mg of tetracycline.
6. Preparation of microcapsule of methyl salicylate of polymer polymer interaction.
7. Preparation of Antacid suspension
8. Preparation of vanishing cream (water based cream)
9. Preparation of liquid paraffin emulsion
10. Preparation of sunscreen cream
11. Preparation of phenobarbitone elixir.
12. Preparation of film coating of tablets.
13. Preparation of enteric coating of tablets.
14. Preparation of antidandruff shampoo.
15. Preparation of cold cream (Oil based cream)
16. Preparation of non staining iodine ointment.
17. Formulation of lubricating jelly.
18. Formulation & preparation of deodorants /antiperspirants.
19. Formulation & preparation of shaving cream.
20. Formulation & preparation of lipsticks.
21. Formulation & preparation of nail enamel.
22. Formulation & preparation of after shave lotion.
23. Formulation & preparation of calamine lotion.
24. Formulation & preparation of mouth washes.
Note: Any other experiment (s) may be included in support of the theoretical aspect of
course.
M.Sc PHARMACEUTICAL CHEMISTRY
(SEMESTER-IV)
PAPER-XIII: MEDICINAL CHEMISTRY –II
Maximum Mark : 100
i)Theory Paper : 70
ii)Internal Assessment : 30
Time: 3 hours
Pass Marks : 35%
Lectures to be delivered : 60
INSTRUCTIONS FOR THE PAPER SETTERS:
The question paper will consist of three sections A, B and C. Section A and B will have four questions
from the respective sections of the syllabus and will carry 07 marks each. Section C will consist of a short
answer / objective type questions, which will cover the entire syllabus uniformly and will carry 28 marks (2
marks each).
INSTRUCTIONS FOR THE CANDIDATES:
1.
Candidates are required to attempt three questions each from sections A and B of the question
paper and the entire section C.
2.
The use of scientific calculators is allowed.
SECTION-A
Structure, stereochemistry, nomenclature, mode of action, specific clinical applications and
structure activity relationships, biosynthesis of naturally occurring compounds and synthesis of
prototypical drugs in each category (Chemical & Pharmacological) for the following classes of
drugs.
Antibacterials: Penicillines, Cephalosporins, Tetracyclines, Aminoglycosides, Chloramphenicol,
Macrolides, Lincomycins, Polypeptide antibiotics, Polyene antibiotics. Sulfonamides and
Sulfones, fluoroquinolines, Trimethoprim and other unclassified antibiotics.
Antimycobacterials: Sulfanilamides, p-Aminosalicyclic acid derivatives , Thioamides, Thiourea
derivatives, Thiosemicarbonazones, Isoniazid, Kanamycin sulfate, Capreomycin, Rifampin,
Pyrazinamide, Anthionamide, Clofazimine, Cyclosporin, Dapsone, Sulfazem. & Antileprotic
agents.
Structure, stereochemistry, nomenclature, mode of action, specific clinical applications and
structure activity relationships, biosynthesis of naturally occurring compounds and synthesis of
prototypical drugs in each category (Chemical & Pharmacological) for the following classes of
drugs.
Anthelmintics: Introduction. Tetrachloroethylene, Piperazines, Gentian violet, Pyrantel pamoate,
Thiabendazole, Mabendazole, baphenium hydroxynaphthoate, Dichlophene, Niclosamide,
levamisole hydrochloride, Tetramisole, Niridazole, Biothional, Antimonypotassium tartarate,
Stibiophen, Sodium Stibiocaptate.
Antiamoebic and antiprotozoal drugs: Emetine hydrochloride, 8-Hydroxyquinoline,
Iodochlorohydroxyquinol, Metronidazole, Diloxanide furoate, Bilamical hydrochloride,
Hydroxystilbamidine isothinate, Pentamidine isothionate, Nifurtimox, Suramin sodium,
Carbarsone,
Glycobiarsol,
Melarsoprol,
Sodium
stibogluconate,
Dimercaprool,
Diethycarbamazine citrate, Centarsone, Acetarsone, Antimony potassium tartarate, Bismuth
sodium thioglycollate, Sulphonamide, Stibiophen, Bismuth sodium thioglycollamate,
Furazolidone.
SECTION-B
Structure, stereochemistry, nomenclature, mode of action, specific clinical applications and
structure activity relationships, biosynthesis of naturally occurring compounds and synthesis of
prototypical drugs in each category (Chemical & Pharmacological) for the following classes of
drugs.
Antiviral agents: Introduction, Screening methodology, Admantane derivatives (Amantadine,
Rimantadine), Idozuridine, Trifluridine, Vidarabine, Ribavarain, Acycloguanosine, Inospiplex,
Methisazone, Zidovudine, Acyclovir, Ganciclovir, Foscarnet, Human interferon.
Antineoplastic agents: Alkylating agents (Nitrogen mustards, Aziridines, Sulfonic acid Esters,
Epoxides, Nitrosoureas, Triazenes, Phosphamides, Mitomycin, comparative activity of alkylating
agents). Antimetaboilities: Antifolates (Methotrexate), Mercaptopurine, Thioguanine, fluorouracil,
Floxuridine, Cytarabine, Azathioprine, antitumor, antibiotics, Dactinomycin, Daunorubricin,
Aclacinomycin, Mithramycin, Bleomycin, Miscellaneous compounds: Cisplatin, Taxol, Gunazole,
Pipobromin, Antitumor alkaloids: Vincristine,vinblastin. Hormones agonist and antgonists:
Steroids, Tamoxifen, Mitotane, Dromastanolone propionate, Testalactone, Megastrol acetate
Immunotherapy.
Structure, stereochemistry, nomenclature, mode of action, specific clinical applications and
structure activity relationships,biosynthesis of naturally occurring compounds and synthsis of
prototypical drugs in each category (Chemical & Pharmacological) for the following classes of
drugs.
Antimalarials: Cinchona alkaloids, 4-Aminoquinolines, 8-Aminoquinolines,
9-Aminoacridines, Biguanides, Pyramidines. Sulfones, Mefloquine and Sulfonamides.
Antifungal drugs: Fatty acids and their derivatives (Propionic acid, zinc propionate, sodium
caprylate, zinc caprylate, undecylenic acid, Zinc undecylenate, Triacetin) . Salicylanilids,
Salicyclic acid, Tolnaftate, p-chloromethoxylenol, Acrisocrin, Fluconazole, Itraconazole,
Haloprogin, Clotrimazole, Econazole, Miconazole, Ketoconazole,Flucytosine, Griseofulvin,
Polyene antibiotics (Nystatin, Amphoetericin-B), Chlorophenesin, Dithranol.
Diagnostic Agents and Organic Pharmaceutical Aids: Diagnostic agents: Introduction,
Radiopharmaceuticals, Pharmacopoeial examples of therapeutic & diagnostic agents. Precaution
& safety measures for handling & disposing.
Books Recommended:
1.
Wilson and Gisvolds Textbook of Organic Medicinal and Pharmaceuticals
Chemistry, 8th edition, edited by R.F. Deorge, J.B. Lippincott Company,
Philadelphia, 1982.
2.
Pharmaceutical Chemicals in Perspective. B.G. reuben and H.A. Wittcoff, John
Wiley & Sons, New York, 1989.
3.
W.C. Foye, Principles of Medicinal Chemistry, Lea & Febiger, Philadelphia,
U.S.A.
Suggested Readingss:
1.
Strategies of Organic Drug Synthesis and Design, D. Lendnicer, John Wiley and
Sons, New York. 1998.
M.Sc PHARMACEUTICAL CHEMISTRY
(SEMESTER-IV)
PAPER-XIV: DRUG DESIGN AND DRUG DEVELOPMENT-II
Maximum Mark : 100
i)Theory Paper : 70
ii)Internal Assessment : 30
Time: 3 hours
Pass Marks : 35%
Lectures to be delivered : 60
INSTRUCTIONS FOR THE PAPER SETTERS:
The question paper will consist of three sections A, B and C. Section A and B will have four questions
from the respective sections of the syllabus and will carry 07 marks each. Section C will consist of a short
answer / objective type questions, which will cover the entire syllabus uniformly and will carry 28 marks (2
marks each).
INSTRUCTIONS FOR THE CANDIDATES:
1.
Candidates are required to attempt three questions each from sections A and B of the question
paper and the entire section C.
2.
The use of scientific calculators is allowed.
SECTION-A
Role of Biotechnology in Drug Discovery : Introduction, , production of Human Proteins, New
therapeutics from Recombinant DNA technology , Protein engineering & Site-directed
mutagenesis, Genetically engineered drug discovery tools ,Natural Proteins, as leads for
structurally modified proteins : The Second Generation of Products from Biotechnology,
Examination of the Structure and Function of Proteins as Tools for the Evaluation of pathological
processes: The Third Generation of Products from Biotechnology.
Designs of Enzyme inhibitor: Mechanism of enzymatic catalysis. Transition state analogs as
enzyme inhibitors. Kinetics of irreversible enzyme inhibition. Design of Reversible and
irreversible enzyme inhibitors with following examples: chymotrypsin, Subtilison, Elastase,
Pepsin,Cholinerterase, Deaminases. Carboxypeptidase. Glutamin synthetase . Trisophosphate
isomerase, Aldolase, Enolase, Decarboxylases, Lysozyme and other glycosyl transferring
enzymes. Creatine Kinase, adenylate Kinases. Asparatate trancarbamolyase. Natural products as
enzyme inhibitors. Penicillin, cephalosporin, Leupeptin. Nojrimycin, Pentastatin, Captopril,
Sulphonamids.
SECTION-B
Computer Aided Drug Designing: Computer requirement hardware, software, Data base and
information retrieval techniques. Graphical description of chemical structure. Molecular
interactions and interactive graphics. Introduction of molecular mechanics, molecular dynamics &
quantum mechanics (semiempirical & ab initio methods).Modelling in medicinal chemistry-uses
and limitations. Logico structural approaches. Activity feature selection within a group of
compounds, Activity profile selection.
IPR: Advantages of Patenting, Types of patents, brief introduction of patenting process.
Search for better and Safer Drugs: Impact of External Factors-The Social, Financial, and
Working Environment : Drug Therapy and Public opinion, Drug Research and Financial
Constraints, Working Climate for Innovative Drug Research.
Books Recommended:
1.
The Organic Chemistry of Drug Design and Drug Action, by R. B. Silverman,
Academic Press, 1992.
2.
Drug Designs – A series of monographs in medicinal chemistry edited by A.J.
Ariens. Ist edition, Vol. I, II, V, VIII & IX (only relevant chapters).
3.
Comprehensive medicinal chemistry. Peragmon Press. 1990, Vol. 4.
4.
Modern Drug Research, Paths to Better and Safer Drugs, Medicinal research
series, volume 12, edited by Yvonne Connolly Martin, Eberhard Kutter, Vokhard
Austel.
Suggested Readings:
1.
Medicinal Chemistry for 21th century edited by C. G. Wermuth, Blackwell
Scientific Publications, 1997.
M.Sc PHARMACEUTICAL CHEMISTRY
(SEMESTER-IV)
PAPER-XV: PHARMACEUTICAL TECHNOLOGY-II
Maximum Mark : 100
i)Theory Paper : 70
ii)Internal Assessment : 30
Time: 3 hours
Pass Marks : 35%
Lectures to be delivered : 60
INSTRUCTIONS FOR THE PAPER SETTERS:
The question paper will consist of three sections A, B and C. Section A and B will have four questions
from the respective sections of the syllabus and will carry 07 marks each. Section C will consist of a short
answer / objective type questions, which will cover the entire syllabus uniformly and will carry 28 marks (2
marks each).
INSTRUCTIONS FOR THE CANDIDATES:
1.
Candidates are required to attempt three questions each from sections A and B of the question
paper and the entire section C.
2.
The use of scientific calculators is allowed.
SECTION-A
Good manufacturing practices :
Current good manufacturing practices applied to
manufacturing, processing, packaging and holding of drugs.
ICH guidelines : Need, for I CH norms, steps involved in I CH process and introduction to
various guidelines . Discussion on I CH guidelines for testing stability of drug products.
Sterilization Methods : Introduction to various methods of sterilization- dry heat, moist heat,
gaseous and radiation.
Parenteral Dosage forms : Preformulation factors, concept of sterile room –design and
maintenance, aseptic processing. Water for injection and its properties, pyrogen and particulate
matter testing, isotonicity and its adjustment. Aqueous and non-aqueous vehicles for injectable
preparations. Containers (glass and polyethylene) and closures for injectables and their evaluation.
SECTION-B
Modified Release Dosage Forms : Basic characteristics of sustained, controlled, delayed release
oral dosage forms.Factors influencing design and performance of oral MR dosage forms.
Approaches used for designing modified release oral dosage forms. Examples of ingredients used
and their characteristics. In vitro and in vivo evaluation of drug release and IVIC correlation.
Novel drug delivery systems: Brief introduction with respect to advantages and limitations of
transdermal, vesicular (liposomes, niosomes), osmotic pumps gastro-retentive dosage forms.
Aerosols: Advantages and limitations of aerosol drug delivery. Types of aerosol delivery systems.
Formulation ingredients, and evaluation of finished aerosols.
BOOKS RECOMMENDED
1.
S.H. Wiling, M. M., Tuckerman and W.S. Hitchings, Good Manufacturing Practice
for Pharmaceuticals, Marcel Dekker Inc., New York, U.S.A., 1982.
2.
3.
4.
5.
J.R. Robinson and V.H. Lee (eds.), Controlled Drug Delivery: Fundaments and
Application , 2nd edition, Marcel Dekker Inc., New York, U.S.A. 1987.
J.I. Wells. Pharmaceutical Preformulation: The physiological properties of Drug
Substances, Ellis Horwood, Chicheater, U.K. 1987.
Y.W. Chien (eds.), Novel Drug Delivery Systems, Marcel Dekker Inc., New York,
U.S.A., 1992.
N.K. Jain (eds.), Controlled and Novel Drug Delivery, CBS Publishes and
Distributiors , New Delhi, India, 1997.
M. Sc. PHARMACEUTICAL CHEMISTRY
(SEMESTER-IV)
Practical Paper—VII: Synthetic Medicinal Chemistry
Time: 4 hours
M. marks: 100
Total practical hours: 60
Suggested Experiments
Preparation/multistep synthesis, purification and spectroscopic characterization of organic
pharmaceuticals and intermediate given below: Acetanilide, Aspirin, Barbituric acid , Hippuric acid,
3,4-dihydro-3-(P-methyl-1phenyl)-1-(2H)-Benzoxazine, Diketoperazine, Paracetamol, thenacetin,
Antipyrene, 2-amino-5-bromopyridine, Nitrazepam, Azo sulfonamides, sulfanilamide, Sulfathiazole,
Diphenyhydantoin , Phenylbutazone, Nifedipine, Alcofenac, Baclofen, Brimindiene, Tolmetin,
procarbazine, Ketoprofen, Amphetamine, Aminopyrine,tetrahydroisoquinolines.
Note: Any other experiment (s) may be included in support of the theoretical aspect of course.