JAWAHARLAL NEHRU TECHNOLOGICAL UNIVERSITY HYDERABAD

Course Objective

The course contents of Unit I and Unit II are mainly aimed at enzyme inhibitors for

the treatment of different CNS and CVS diseases. Unit III contents are aimed to have advanced knowledge of the developments of antipsychotic agents. The remaining contents are aimed to design prodrugs, peptidomimetic agents and recombinant DNA products.

Course Outcome

The student would be in a position to involve in the development of different

enzyme inhibitors, prodrugs and also equipped with different biotechnological techniques of recombinant DNA products.

UNIT - I

Enzyme Inhibitors I: A detailed study of the following types of enzyme inhibitors, related drugs and their pharmaceutical significance:

• a) Prostaglandin Synthetase (Cycloxygenase & Lipoxygenase Inhibitors)
• b) Phosphodiesterase (PDE) Inhibitors
• c) Carbonic Anhydrase Inhibitors.
• d) B- Secretase.

UNIT - II

Enzyme Inhibitors II:

• a) Angiotensin Converting Enzyme (ACE) Inhibitors
• b) Acetyl Cholinesterase (Ach E) Inhibitors.
• c) HMG-CoA inhibitors
• d) Protease inhibitors

UNIT - III

Antipsychotic Agents: Role of Dopamine, Serotonin, Glutamate and their receptors. SAR and Pharmacokinetics of Ticyclic Neuroleptics, Butyrophenones and Benzamides. A brief account of non – benzodiazepine agonist.

UNIT - IV

Peptidmimetic agents & Prodrugs

• a) Physiological role of peptides, Endogenous peptide transmitters & function, cyclosporin and oxytocin
• b) Prodrugs belong to esters, Lactones, amides, hydrazides and azo compounds. Targeted prodrug, bioprecurror of prodrugs

UNIT - V

Biotechnologically produced drugs: Biotechnology of Recombinant DNA, Process of Recombinant proteins, Immunogencity of biotechnologically produced drugs. Recombinant drug products: Hormones, cytokinins, interferons, Interleukins, enzymes, vaccines and monoclonal antibody drugs.

RECOMMENDED BOOKS:

• 1. Berger’s Medicinal Chemistry and Drug Design. 6th Edition
• 2. Korolkovas Essentials of Medicinal Chemistry
• 3. William O Foye Medicinal Chemistry
• 4. Lednicer, Organic Chemistry of Drug Synthesis
• 5. Ariens, Drug Design, Academic Press
• 6. Purcell Strategies of Drug Design
• 7. Corwin, Hansen Comprehensive Medicinal Chemistry
• 8. Richard B. Silvermann, Org. Chemistry of Drug Design and drug Action
• 9. Smith and Williams, Introduction to principles of Drug Design – Harwood Academy Press
• 10. Gyorgy Keri &IstdanToth Molecular Pathomechanism and New Trends in Drug Research, Taylor & Francis Pub
• 11. Thomas Nogrady, Medicinal Chemistry. A biochemical Approach, Oxford Univ. Press. M.Pharm I Year II Sem (Pharmaceutical Chemistry)