Syllabus
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Course Code: CHEM 402 Course Name: Pharmaceutical Chemistry Special-IV |
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| MODULE NO / UNIT | COURSE SYLLABUS CONTENTS OF MODULE | NOTES |
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| 1 | Drug Design Introduction, Procedure followed in drug design-Screening of natural compounds, isolation, purification, structure determination, Search for lead Compounds, Molecular Modification of Lead Compound, prodrugs- utility, drug latentiation, carrier linked and bioprecursor prodrugs, Prodrugs of compounds containing alcohols, carboxylic acids, amines and carbonyl groups, drug synergism, hard and soft drugs. Structure-Activity Relationship (SAR), isosterism, Bioisosterism, Factors affecting Bioactivity, Theories of Drug Activity; Occupancy theory, Rate theory, Induced Fit theory |
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| 2 | Quantitative structure-activity relationships (QSAR) Development of QSAR, Physicochemical parameters- Lipophilicity parameter, Polarizability, Electronic parameter, Ionization Constants, steric Parameters- Taft’s steric factor, molar refractivity, Verloop steric parameter, chelation parameters, Surface activity parameter, redox potential, hansch analysis, Craig plot, Topliss Scheme, Free-Wilson Approach. Co-Enzyme Chemistry Cofactors as derived from vitamins, coenzymes, prosthetic groups, apoenzymes. Structure and biological functions of coenzyme A, thiamine pyrophosphate, pyridoxal phosphate, NAD+, NADP+, FMN, FAD, Mechanisms of reactions catalyzed by the above cofactors. |
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| 3 | Combinatorial Chemistry Introduction to Combinatorial chemistry, Combinatorial approaches, solid phase techniques, liquid phase synthesis, Chemical Peptide and small molecular libraries, split synthesis and parallel synthesis- applications and methodology, deconvolution, Combinatorial Organic Synthesis. High throughtput screening (HTS), Planning and designing a combinatorial synthesis-scaffolds, X-ray crystallography, docking procedures. |
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| 4 | Enzymes Introduction and historical perspective, chemical and biological catalysis, remarkable properties of enzymes like catalytic power, specificity and regulation. Nomenclature and classification, extraction and purification. Fischer's lock and key and Koshland's induced fit hypothesis, concept and identification of active site by the use of inhibitors, affinity labeling. Enzyme kinetics, Michaelis-Menten and Lineweaver-Burk plots. Enzyme inhibitors- reversible, irreversible, suicide inhibitors. Mechanism of Enzyme Action. Transition-state theory, orientation and steric effect, acid-base catalysis, covalent catalysis, strain or distortion. |
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