Master of Pharmacy - Nagpur University

5. P.S. Kalsi, 2006, Stereochemistry, Conformation and Mechanism, 6 th edition, New Age
International (P) Limited, Publishers, New Delhi.
6. D. Nasipuri, 2003, Stereochemistry of Organic Compounds – Principles and
Applications, 2 nd edition, New Age International (P) Limited, Publishers, New Delhi.
7. Laszlo Kurti & Barbara Czako, Strategic application of named reaction in organic
synthesis, Elsevier Academic Press.
8. Peter Sykes, 1985, A Guidebook to Mechanism in Organic Chemistry, 6 th edition,
Longmann Scientific and Technical, Copublished with John Wiley & Sons, Inc, New
York.
9. G.R. Stephenson, 1996, Advanced Asymmetric Synthesis, 1 st edition, Blackie
Academic and Professional, London
Subject code: MPC-S10
Subject: ADVANCED PHARMACEUTICAL CHEMISTRY-III
THEORY: 60 Hours (4 hrs. /week)
1. GENESIS OF NEW DRUGS:
i) A brief review of the following topics: sources of new drugs; leads from natural
products; molecular modifications; random screening; high thought put screening; insilico
screening; structural features and pharmacological activity; prodrugs; soft drugs; isosterism.
selective optimization of side activities (SOSA) approach, , new use for old drugs – An
illustrative study with suitable examples
ii) A brief account of drug discovery by recombinant DNA technology.
2. PRINCIPLE OF DRUG DESIGN:
Analogue synthesis versus rational design; discovery of lead compounds, Pharmacophoric
identification, Prodrugs and soft drug. Physicochemical properties in relation to drug action;
metabolic transformation of drugs and its role in development of new drug molecules.
QSAR in drug design.
a) Physical properties related to potency.
b) Calculation, measurements and significance of various parameter used in QSAR –
(Lipophilicity, steric, Electronic effects). c) applications of Hansch Analysis.
Computers in drug design:
Introduction; computer graphics and molecular visualization; computational chemistry
overview, force field methods; geometry optimization; conformational searching; molecular
dynamics simulations; quantum mechanics; structure based drug design and Pharmacophore
perception, predictive ADME.
3. MEDICINAL CHEMISTRY OF
a. Antiviral Agents and agents under development of HIV infection.
b. Immunosuppressant and Immunostimulants.
c. Agents used in Neurodegenerative disease Like Alzheimer‟s and Parkinsonism.
d. GABAnergic Agonists.
e. Antidiabetic agents like Peroxisome Proliferator Activated Receptors inhibitors,
Dipeptidyl Peptidase 4 (DPP 4) Inhibitors like Sitagliptin, Vildagliptin, Protein Tyrosine
Phosphatase 1 B (PTP 1 B).
f. Antihypertensives like Direct Renin Inhibitors e.g. Aliskiren
NOTE: “A study of” includes an account of their origin and development, classification,
structures, mechanism of action, SAR, uses and toxicity.
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