Advanced Medicinal Chemistry

THEORY 1.

Drug discovery: Stages of drug discovery, lead discovery; identification, validation and diversity of drug targets.

Biological drug targets:

Receptors, types, binding and activation, theories of drug receptor interaction, drug receptor interactions, agonists vs antagonists, artificial enzymes.

Hrs Prodrug Design and Analog design:

a) Prodrug design: Basic concept, Carrier linked prodrugs/ Bioprecursors, Prodrugs of functional group, Prodrugs to improve patient acceptability, Drug solubility, Drug absorption and distribution, site specific drug delivery and sustained drug action. Rationale of prodrug design and practical consideration of prodrug design.

b) Combating drug resistance:

Causes for drug resistance, strategies to combat drug resistance in antibiotics and anticancer therapy, Genetic principles of drug resistance.

c) Analog Design: Introduction, Classical & Non classical, Bioisosteric replacement strategies, rigid analogs, Hrs alteration of chain branching, changes in ring size, ring position isomers, design of stereo isomers and geometric isomers, fragments of a lead molecule, variation in inter atomic distance.

a) Medicinal chemistry aspects of the following class of drugs Systematic study, SAR, Mechanism of action and synthesis of new generation molecules of following class of drugs:

a) Anti-hypertensive drugs, Psychoactive drugs, Anticonvulsant drugs, H1 & H2 receptor antagonist, COX1 & COX2 inhibitors, Adrenergic & Cholinergic agents, Antineoplastic and Antiviral agents.

b) Stereochemistry and Drug action: Realization that stereo selectivity is a pre-requisite for evolution. Role of chirality in selective and specific therapeutic agents.

Case studies, Enantio selectivity in drug adsorption, metabolism, distribution and elimination.

Hrs Rational Design of Enzyme Inhibitors Enzyme kinetics & Principles of Enzyme inhibitors, Enzyme inhibitors in medicine, Enzyme inhibitors in basic research, rational design of non-covalently and covalently binding enzyme inhibitors.

Hrs Peptidomimetics Therapeutic values of Peptidomimetics, design of peptidomimetics by manipulation of the amino acids, modification of the peptide backbone, incorporating conformational constraints locally or globally. Chemistry of prostaglandins, leukotrienes and thromboxones.

Hrs