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Medicinal Chemistry: Course Outline-(904)

Medicinal chemistry is the chemistry discipline concerned with the design, development and synthesis of pharmaceutical drugs.

Course Outline

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

Relevant Books