Natural
products as leads for new drugs:
Introduction/history, approaches to discovery and development of natural
products as potential new drugs selection and optimization of lead compounds
for further development with suitable examples from antibiotics, CNS, and
cardiovascular agents.
Alkaloids: Introduction and general methods of structure
elucidation.
From
opium: morphine-structural elucidation, development of morphine analogues and
morphine antagonists.
From
Rauwolfia: Reserpine-structural eludication, structural modifications and uses.
From
vinca rosea: vincristine and vinblastine - structural modification, semi
synthetic derivatives, and uses.
Steroids: Introduction, nomenclature, stereochemistry of
steroids. Source and structure elucidation of cholesterol and diosgenin.
Structures,
structural modifications and therapeutic uses of steroidal anti-inflammatory
agents and antifertility agents.
Polypeptides
and proteins: introduction and
general methods of separation, general methods of degradation and end group
analysis, general methods of synthesis of peptides. Primary, secondary,
tertiary and quaternary structure of proteins; chemistry of insulin.
Miscellaneous
compounds: Structure, structural
modifications, mechanism of action and therapeutic uses of a) taxanes b)
camptothecin c) artemisicin e) ginkolides and f) gymnemic acids.