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Medicinal Chemistry

Indian Institute of Technology Madras via NPTEL

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Overview

The main objective of this course is to familiarize students with the fundamental concepts of drug discovery and development. The course is intended for students who have a background in chemistry and interested in the process of drug discovery. The intended outcome is to train students on various aspects of new drug discovery/development, drug screening, target identification, lead discovery, optimization and the molecular basis of drug design and drug action.

INTENDED AUDIENCE:
Third year undergraduates of B.Sc. Chemistry; M.Sc. Chemistry students and doctoral students

PREREQUISITES: Any student who has done basic organic chemistry and has some knowledge of biochemistry with an interest in drug discovery.

Syllabus

Week 1  :  An overview of drugs and drug targets; structure of a cell; intermolecular binding forces; classification of drugs.
Week 2  :   Principles of enzyme structure, catalysis and inhibition in drug discovery: Enzyme mechanisms overview; enzyme catalysis and inhibition in drug discovery; reversible and irreversible inhibitors; transition-state inhibitors; case studies
Week 3  : Principles of enzyme structure, catalysis and inhibition in drug discovery: Enzyme mechanisms overview; enzyme catalysis and inhibition in drug discovery; reversible and irreversible inhibitors; transition-state inhibitors; case studies,Receptors function and ligand binding interactions; Ion channel receptors; kinase-linked receptors; G-Protein coupled receptors, drug-receptor interaction; dose-response curves; case studies
Week 4  :  Receptors function and ligand binding interactions; Ion channel receptors; kinase-linked receptors; G-Protein coupled receptors, drug-receptor interaction; dose-response curves; case studies
Week 5  :  Nucleic acids structure and function; DNA Interactive agents and chemotherapy: DNA binding agents; intercalation and alkylation; DNA strand breakers; case studies
Week 6  :  Synthetic methods in medicinal chemistry: Combinatorial and parallel synthesis: solid phase techniques, mix and split method in combinatorial synthesis; dynamic combinatorial synthesis; solid phase synthesis; diversity-oriented synthesis.
Week 7  :  Lead discovery; Bioassays; drug targets; Lead Modification; optimization; pharmacophore; homologation; bioisostere; chain branching; Electronic effects; Lipophilicity; Structure-Activity Relationships; Quantiative-structure activity relationships (QSAR). 
Week 8  :  Lead discovery; Bioassays; drug targets; Lead Modification; optimization; pharmacophore; homologation; bioisostere; chain branching; Electronic effects; Lipophilicity; Structure-Activity Relationships; Quantiative-structure activity relationships (QSAR). 
Week 9  :  Drug metabolism and pharmacology: Analytical methods in metabolism; Phase I and Phase II transformations; Absorption, distribution, metabolism and excretion (ADME); bioavailability; pre-clinical and clinical development; therapeutic index and therapeutic window.
Week 10  :  Prodrugs and drug delivery systems: Use of prodrug systems; prodrugs for stability, solubility and slow release; overview of drug delivery
Week 11  :  Drug resistance mechanisms and synergism: Mechanisms of drug resistance; circumventing drug resistance; drug synergy
Week 12  :  Drug resistance mechanisms and synergism: Mechanisms of drug resistance; circumventing drug resistance; drug synergy

Taught by

Prof. Harinath Chakrapani

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