PY8010 - ADVANCED MEDICINAL CHEMISTRY (Syllabus) 2017-regulation Anna University

PY8010 - ADVANCED MEDICINAL CHEMISTRY (Syllabus) 2017-regulation Anna University

PY8010

ADVANCED MEDICINAL CHEMISTRY

 LPTC

3003

OBJECTIVES: The content of this syllabus is designed
• To understand the role of enzyme induction and inhibition for drug biotransformation
• To cater essential features of pharmacophores to enable a ligand molecule to interact with a specific target receptor.
• To understand the mode of action and structure activity relationship of Chemotherapeutic agents, Amino acids, peptide, nucleotides and related drugs and Steroids and related drugs

UNIT I

BIOTRANSFORMATION OF DRUGS

9

Protein Binding, Prodrug approach, Soft Drug approach, enzymes responsible for biotransformation, microsomal and non-microsomal mechanisms. Factors influencing enzyme induction and inhibition.

UNIT II

PHARMACOPHORE CONCEPT

9

Methods of conformational search used in pharmacophore mapping. Comparison between the popular pharmacophore methods like Catalyst/HipHop, DiscoTech, GASP with practical examples. De Novo drug design techniques: Receptor/enzyme cavity size prediction. Predicting the functional components of cavities, designing drugs fitting into cavity.


UNIT III

CHEMOTHERAPEUTIC AGENTS

9

Synthetic procedures of selected drugs, mode of action, uses, structure activity relationship including Physico-Chemical properties of Antitubercular, Antimalarial, Antifungal, and Antiamoebic drugs.

UNIT IV

PEPTIDES, NUELEOTIDES AND RELATED DRUGS

9

Synthetic procedures of selected drugs, mode of action, uses, structure activity relationship including Physico-Chemical properties of the following classes of drugs Thyroid and Anti thyroid drugs, Insulin and oral hypoglycaemic agents.

UNIT V

STEROIDS AND RELATED DRUGS

9

Synthetic procedures of selected drugs, mode of action, uses, structure activity relationship including Physico-Chemical properties of the following classes of drugs Steroidal nomenclature and stereochemistry, androgens and anabolic agents, estrogens, and progestational agents, adrenocorticoids.

TOTAL : 45 PERIODS

OUTCOMES:
• The student would be equipped with the advanced knowledge of identification of different targets in different diseases.
• The student will be able to involve in drug discovery programmes including lead identification, design of pro drug and their metabolic pathways.
• The student will be able to interpret structure-activity relationships and fundamental principles governing the molecular interactions of a drug with its target.

TEXT BOOKS:
1. Donald J. Abraham, David P. Rotella (Eds.,), Burger’s Medicinal Chemistry and Drug Discovery, Vol. I-VIII, 7th Edition, John Wiley and Sons, Inc., New Jersy, 2010.
2. Wilson and Gisvold, Textbook of Organic Medicinal and Pharmaceutical Chemistry, 12th Edition, Lippincott Williams & Wilkins –Philadelphia, 2010.
3. William O Foye, Thomas L Lemke, David A Williams Foye’s Principles of Medicinal Chemistry, 7th Edition, Wolters Kluwer Health Adis (ESP) Publisher, 2012.
4. Daniel Lednicer, Lester A. Mitscher (Eds.), The Organic Chemistry of Drug Synthesis, Vol. I-VII, Wiley Publisher, 2007.

REFERENCES:
1. Ariens, Drug Design: Medicinal Chemistry, Volume I-X, Academic Press, 2009.
2. Corwin, Hansen, Comprehensive Medicinal Chemistry III, 3rd Edition, Elsevier, 2017.
3. Richard B. Silvermann, Mark W. Holladay, The Organic Chemistry of Drug Design and Drug Action 3rd Edition, Academic Press, 2014.
4. H. John Smith, Hywel Williams, Introduction to principles of Drug Design, CRC Press, 2005.
5. Camille Wermuth, David Aldous, Pierre Raboisson, Didier Rognan, The Practice of Medicinal Chemistry, 4th Edition, Elsevier Publications, 2001

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