Applied Medicinal Chemistry: Course Outline (904)

Introduction to medicinal chemistry

• General properties
• Chemistry
• Biological action

Structure activity relationship and therapeutic applications of the following

• Anti-septics
• Sulphonamides
• Antimalarials
• Anthelmintics
• Diuretics
• Anti-tubercular drugs
• Antiviral drugs and immunosuppressant agents
• Alkaloids
• Vitamins
• Hormones
• Anti-neoplastic agents
• Sedatives and hypnotics
• Anesthetics
• Local anesthetics
• General anesthetics
• Analgesics and antipyretics

Cell membrane chemistry

• Receptors
• Drug receptor interaction
• G-protein coupled receptors
• Ion channel linked receptors
• Ligand gated ion channels (LGICs)

Ligand-Receptors theories

• Clarks occupancy theory
• Rate theory
• Induced fit theory
• Macromolecular perturbation theory and activation aggregation theory

Drug design tools

Conventional methods of drug design

• Lead
• Discovery of lead
• Lead optimization
• Objective of lead optimization
• Pharmacophoric identification and analog approach of drug designing
• Prodrug Concept for drug design
• Drug targeting and antibody directed enzyme prodrug therapy (ADEPT)
• Soft drug design

Rational design of enzymes inhibitors

• Design of non-covalently binding enzymes inhibitors:
• Rapid reversible inhibitors
• Slow
• Tight and slow-tight inhibitors
• Transition state analogues
• Multisubstrate inhibitors
• Current developments with respect to the inhibition of the different enzymes