Design Synthesis and Biological Evaluation of Small Bioactive Heterocycles as Antituberculosis Agents

Abstract

Tuberculosis, a major contagious air-borne disease, kills millions in a year. Many of the existing anti-tubercular drugs suffer from resistance problems. They are highly bactericidal but later on due to several factors like poor patient compliance, incomplete therapy, etc. leads to treatment relapse. Several measures in terms of research have been explored in identifying molecules to combat the disease. However, drugs in clinical trials such as delamanid, pretomanid, and bedaquilline have given a greater relief after a long time to manage the multidrug-resistant strains. The mechanism of action of these drugs were found to be inhibiting keto mycolic acids, methoxy mycolic acids, actively replicating Mycobacterium tuberculosis, and ATP synthase respectively. These drugs has proven to have greater efficacy. newlineThe current research focus is on identifying new leads with a novel mechanism of action either to acts solely or as a combined regimen to express its synergistic action in inhibiting the organism. The current trends in the drug discovery process utilize CADD which plays a crucial role in drug discovery and development. The target identification is important in terms of mechanism in inhibiting the organism and addressing the resistance problem newline newline