Unit 1: Introduction to Pharmaceutical Chemistry(10 Hrs)Introduction to Pharmaceuticals, Historical development, Classification drugs, Nomenclature of Pharmaceuticals.Drug discovery and development process, Sequence of events after drug administration, List of physico-chemical properties related to drug action, Clinical Chemistry and the importance of fundamental chemistry concepts and analytical techniques Unit 2: Drug-Target Interactions(8 Hrs)Structural Effects on Biological Action, Role and types of chemical bonding interactions between drug and target, binding of neurotransmitters to their receptors, Solubility, partition coefficient, dissociation constant, hydrogen bonding, ionization, drug shape, surface activity, complexation, protein binding, molar refractivity.Enzyme, receptors, nuclei acid, protein, lipid as drug targets.Unit 3: Basics of Drug Action(8 Hrs)Energy: Energy concept and its importance in drug action. First, Second and Third laws of thermodynamics and the principles derived from these laws which are of significance to drug action.Thermodynamics: Free energy and Relationship between thermodynamics and statistics. Importance of chemical potential in drug action. Thermodynamic cycle. Statistical thermodynamics in predicting the structure of biomolecules and their interaction with drug molecules. Macromolecular vs. micromolecular correlation using thermodynamics and statistical thermodynamics.Unit 4: Influence of Stereochemistry on Drug Action(8 Hrs)Stereoisomers, Stereochemistry of unsaturated compounds, Enantiomers, Diastereomers, Partition coefficients.Bioisosterism stereochemical aspects of drug action, Realization that stereoselectivity is a pre-requisite for evolution; Role selective and specific therapeutic agents; Case studies; Enantioselectivity in drug absorption, metabolism, distribution and eliminationUnit 5: Chemical Aspects of Drug Metabolism(8 Hrs)Introduction, Effects of chemical structure on Phase I oxidative, reductive, and hydrolytic reactions, Effects of chemical structure on phase II conjugative reactions (COMT and PNMT-catalyzed methylation, acetylation, sulfation, glucuronidation, amino acid conjugation, mercapturic acid formation), Sites of metabolism, Metabolic pathways of selected common drugs, Metabolites identified for a new anticancer drug, Imatinib.
