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.