Concept and definition of Pharmacophore. Pharmacodynamics and Pharmacokinetics – . Drug targets: enzymes and receptors. Competitive, non-competitive and allosteric inhibitors, transition-state analogs and suicide substrates. Nucleic acids as drug targets: reversible DNA binding agents, DNA alkylating agents and DNA strand breakers. ADMET of drugs: Factors affecting Absorption, Distribution, Metabolism, Elimination and Toxicity.

Drug Discovery, Design and Development. Structure-activity relationships: Strategies in drug design. QSAR and combinatorial synthesis. Optimization of drug-target interactions and access to drug targets. Pro-drugs and drug delivery systems.

Illustration of drug development through specific examples: a) Antibacterials: sulfonamides and penicillins b) Antivirals: case studies with inhibitors of reverse transcriptase (nucleoside reverse transcriptase- and non-nucleoside reverse transcriptase inhibitors) and protease inhibitors. c) Anticancer agents: antimetabolite-based approaches, those which affect signaling pathways or structural proteins such as tubulin. Drug resistance, Drug synergism and combination therapy.

References:

1. Patric, G. L., An Introduction to Medicinal Chemistry. 3rd ed.; Oxford University Press: 2005.
2. Silverman, R. B., The Organic Chemistry of Drug Design and Drug Action. 2nd ed.; Academic Press: 2004.
3. Williams, D. A.; Lemke, T. L., Foye’s Principles of Medicinal Chemistry. 5th ed.; Wolters Kluwer Health (India) Pvt. Ltd.: 2006.