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Exploring Novel Benzopyran Derivatives as Antitubercular Agents
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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.
Title: Exploring Novel Benzopyran Derivatives as Antitubercular Agents
Description:
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.
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