CY 6108 : Medicinal Chemistry

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.


  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.