SYNTHESIS AND SYNTHETIC TRANSFORMATION OF HETEROCYCLIC COMPOUNDS AND NATURAL PRODUCTS IN SEARCH OF USEFUL THERAPEUTIC AGENTS

Abstract

This dissertation synthesis and synthetic transformation of different classes of heterocycles such as 2,5-disubstituted-1,3,4-oxadiazoles, 2-substituted-1,3, thiazolidines-4-carboxylic acid, 2-aminothiophenes and their analogs in search of important therapeutic agents. Some 2,5-disubstituted-1,3,4-oxadiazoles have been synthesized and found to be novel tyrosine inhibitors. 2-Substituted-1,3-thiazolidines-4-carboxylic acid and 2-aminothiophenes have been discovered as potential urea inhibitors. Some hydrazides were screened for their in vitro leishmanicidal activity and have been found to have very exciting activities. Leishmaniasis, which is endemic to eighty two countries throughout the world and is most frequent in south east region, has been reviewed extensively. This dissertation also deals with a new emerging microwave assisted synthetic methodology and its use in the synthesis of various compounds of therapeutic importance. In addition to above all this dissertation describes the exciting four step “total synthesis of (4S,5R)-(+)-L-Factor, also called as (SS)-5-[(IR)-1-hydroxyhexy1]dihydro-2(3H)-furanone, a proposed autoregulator of anthracycline biosynthesis” from commercially available L-glutamic acid [(S)-(+)-glutamic acid]. The chemistry of the CsF-Celite has also beenexploited because it can serve as an excellent solid base for converting carboxylic acid into their corresponding esters with alkl halides. A methodology based on CsF-Celite has also been developed to synthesize y-lactone skeleton.