CHEM 655 - Introduction to Biomedicinal Chemistry

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A survey of (a) principles and methods of drug design, including modern rational approach aided by computers, disease models, natural products, analogue synthesis and pharmacophore identification; (b) physio-chemical principles of drug action, including solubility; partition co-efficients; surface interactions; stereo-chemical, electronic and quantum chemical factors; chemical bonding; and quantitative structure activity relationships (QSAR); (c) receptor concept of drug action, including nature, definition, characterization, models and classical theories of receptor function; (d) mechanisms of drug action, including enzyme stimulation, inhibition and regulation; (e) drug distribution, metabolism and inactivation, including bioavailability, biotransformations, chemical and metabolic stability; pharmaco-kinetic variability and design of pro-drugs; (f) case studies selected from a list of anti-tumor, analgetic, anti-microbial, anti-cholinergic, antiadrenergic, psychoactive and cardiovascular drugs; and (g) current status and future impact in drug development, including protein therapeutics, gene therapy, anti-sense drugs, cytokines and drug resistance.
Prerequisite: Prerequisite: Consent of instructor.