Studies on Diversity Oriented Synthesis of Bioactive Compounds

Abstract

Diversity-oriented synthesis (DOS), aims to synthesize a collection of compounds that differ substantially in their molecular structure. The strategy has been proven to be an essential tool for the discovery of small bioactive molecules As a part of the research programme entitled “Studies on Diversity Oriented Synthesis of Bioactive Compounds,” to develop diverse classes of small molecule libraries containing potential biological properties, the present thesis covers the synthesis, chemistry and biological activities of some privileged scaffolds as quinazoline, benzopyran and fused diazoles. The results of these studies are discussed in four chapters as summarized below: First chapter includes a brief review on synthesis, chemistry and biological activities of quinazoline, benzopyran and fused diazoles. Second chapter consists of three sections which describes the details of synthesis and biological activities of novel quinazoline derivatives. The chapter deals with diversity oriented synthesis of a new class of atropisomeric P,N-ligands and a class of novel biologically active 2,4-disubstituted quinazolines as shown below.Third chapter consists of three sections which covers the synthesis and biological activities of some benzopyran derivatives. The chapter deals with diversity oriented synthesis of two scaffolds 2H-chromen- 2-one and 2H-chromene, starting from 2-hydroxybenzaldehyde to biologically active molecules as shown below. Fourth chapter consisting of two sections describes the synthesis and biological activity of fused diazoles. The chapter deals with diversity oriented synthesis of indolizines and benzimidazoles class of fused diazoles and their biological evaluation. Central Drug Research Institute is one of the first and few laboratories that were established in India right after its independence. CDRI is considered to be a pioneer research organization in the field of biomedical research where all the infrastructure and expertise are available to develop a drug right from its concept to market. The thesis work has been carried out from February 2005 to April 2009 at the Division of Medicinal and Process Chemistry, CDRI.