Chemistry of Drug Design and Metabolism




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Prerequisites: CHM 481 

Course Contents

Physicochemical Principles of Drug Action; Partition Coefficients; Receptor-Effector Theories; Role of Second Messengers in Drug Action; Methods of Receptor Isolation, Characterization and Modeling (5)

Principles of Drug Design: Random Screening, Analogue Synthesis, Rational Design, Combinatorial Libraries; Enantiopure Drugs and Regulatory Implications; Theoretical Approaches: QSAR, Topliss Tree, MSA, CoMFA (2)

Neuroactive Drugs: Neurons and Neurotransmitters; Brain-related Disorders and Chemotherapy; Drugs Interacting with Cholinergic, Adrenergic, Dopaminergic and Histaminic Receptors and Receptor-subtypes (5)

Anticancer, Antimalarial, Antiviral, and Cardiovascular Drugs; Emerging Trends in Drug Design: Inhibitors of DNA Topoisomerase and Protein Farnesylation & Prenylation; Gene-Based Medicines (8)

Biopharmaceuticals: Recombinant Proteins as Medicines and Vaccines (2)

Drug Delivery: Passive, Assisted and Vector-Based Delivery of Conventional and Genetic Drugs; Tissue-Specific Delivery of Antitumor Agents (8)

Drug Administration, Distribution, Metabolism and Elimination (ADME); Pathways of Drug Metabolism: Enzymology and Molecular Mechanisms; Detoxification of Diverse Drug Classes; Dose Formulation (10)

Induction and Inhibition of Drug Metabolism; Toxicological Aspects of Metabolism: Metabolic Activation of Environmental Carcinogens and DNA Damage; Drug Pharmacokinetics and Final Body Clearance (2) 



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  • Medicinal Chemistry: A Biochemical Approach, Thomas Nogrady

  • Principles of Medicinal Chemistry, William O. Foye

  • The Pharmacological Basis of Therapeutics: Goodman and Gilman

  • Introduction to Drug Metabolism, G. Gordon Gibson and Paul Skett




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