DRUG DISCOVERY AND DEVELOPMENT

The course focuses on the molecular basis of target-based drug discovery, with emphasis on the biological targets of therapeutic relevance for rational discovery & development of small molecules drugs.

Topics covered through the course are: Principles governing drug-receptor interactions, molecular mechanism of drug-receptor recognition, stereochemistry.
Discovery of Lead compounds, structure-activity relationships.
Rational development of drugs: natural products and existing drugs as chemical scaffolds for the discovery and design of novel therapeutics, analog design, computer-aided rational design, peptidomimetics.
Examples treated in details will be benzodiazepines, opioid analgesics, renin-angiotensin-aldosterone inhibitors, Histamine-2 antagonist, COX-inhibitors and kinase inhibitors. Particular attention will be devoted to the discovery and development of HIV-protease inhibitors and sialidase inhibitors, and in general to the development of antibacterial and antiviral drugs.