Synthesis of New Generation of Antimycobacterial Agents Based on Sugars and Aromatics

Abstract

Medicinal chemistry, an important branch of chemical sciences, serving the mankind by helping them to overcome, conditions unfavorable for their survival has fascinated the scientific community throughout the world. The ingress to the human population of new disease causing agents such as Mycobacterium tuberculosis, HIV, Ebola and SARS and disorders like diabetes and dyslipidemia requires the discovery and development of new drugs to combat them. Not only do diseases like AIDS require drugs that target them specifically, but new therapies are needed for treating ancillary infections which are a consequence of a weakened immune system. One of the prominent disease Tuberculosis (TB) claiming with nearly two million death every year throughout the world and recent challenge of MDR-TB, XDR-TB and HIV/TB synergy has led to declare this disease as global health threat by WHO. Therefore, attempts are being made to develop new antitubercular drugs with a novel and new mode of action. Since the Central Drug Research Institute, Lucknow, is deeply involved in drug discovery and development in India hence, during the course of this thesis several bioactive molecules were synthesized and taken up to accomplish the desired objective of the current studies. The present thesis encompasses the specific objectives, results and discussion of these studies and is divided into five chapters as summarized below: Chapter-1: Collates the data on the recently developed new leads with a brief overview on Tuberculosis its global picture treatment measures, drug targets and future chemotherapeutics. Chapter-2: Dwells with the synthesis of aryl & heteroaryl amines and their bioevaluation as antitubercular agents. Chapter-3: Describes the synthesis of azatricyclodiones & octahydro-benzo [f]isoindoles & their anti-microbial evaluation. Chapter-4: Comprises the green chemistry perspective of one-pot multicompo nent solvent-free synthesis of hexahydro-1H-quinazoline-2-thiones and 8-benzylidene-hexahydro-1H-quinazolin-2-one. Chapter-5: Encompasses the syntheses of 1-O-mannofuranosyl phenolics.