Exploring Novel Benzopyran Derivatives as Antitubercular Agents

Background: Tuberculosis (TB) remains a significant global health concern, necessitating the exploration of novel therapeutic agents. Reported antitubercular activities of previously synthesized benzopyran and other oxygen-containing heterocycles motivate us to synthesize and evaluate the antitubercular potential of benzopyran derivatives. Objective: The aim of this study was to combine two scaffolds; one is coumarin (benzopyran-2-one), and another one is piperazine, as both are found in anti-tubercular derivatives. Methods: Through a four-step synthetic approach, compounds SM1-SM10 were synthesized. These derivatives were subsequently evaluated for their in vitro anti-tubercular potential using the resazurin microtiter assay (REMA), with isoniazid as the standard (MIC 0.25 to 0.5μg/mL). Results: Among the synthesized compounds, SM2 and SM8 demonstrated remarkable antitubercular activity, with MICs of 4 and 6μg/mL, respectively. Notably, these MIC values are considerable for the further development of benzopyran derivatives as potent antitubercular agents. Conclusion: Outcomes underscore the potential of benzopyran derivatives as valuable assets in TB drug discovery, warranting further exploration and development.