Benzopyran-Core as an Antimycobacterial Agent

Abstract

Tuberculosis (TB) is one of the world’s most deadly infectious diseases, causing 1.2 million deaths in 2018. TB is the leading cause of death from a single infectious agent, ahead of HIV/AIDS. The African continent bears the highest global TB/HIV burden and over 50% of TB cases in sub-Saharan Africa are co-infected with HIV. With an estimated 1.7 billion people (23% of the world’s population) with latent TB infection, there is an urgent need to develop drugs that will eradicate or control the disease. Moreover, the emergence of multi-drug resistant tuberculosis (MDR-TB) and extensively drug resistant tuberculosis (XDR-TB) have accelerated the need for new antitubercular agents with novel biological targets and different mechanism of action. Among the wide spectra of heterocyclic compounds, benzopyran derivatives have displayed diverse biological applications. Found in many natural products, this scaffold together with its synthetic analogs has intrigued medicinal chemists to explore its applicability as anti-TB drugs. To further intensify research in this area, there is need to gather the latest information on benzopyrans as antimycobacterial agents. This review presents an overview of recent developments (2000 -2018) in anti-TB applications of benzopyrans, both the synthetic analogs and isolated natural products. The objective of this review is to focus on active benzopyran analogs and structure activity relationship (SAR) analysis. We envisage that this review will be helpful in rational design of potent, less toxic benzopyran-based anti-TB drug candidates. a the of mycobacterial cell wall lipid biosynthesis. oxo-4H-chromene-3-carbonitriles with ethyl cyanoacetate. The compounds were investigated for their antitubercular activity against H 37 Rv at a concentration of 62.5μ g/mL, using the L-J method. In this experiment, compound 29 was the most effective against H 37 Rv strain with 99% inhibition [70].