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Synthesis and evaluation of nitrofuranyl methyl N-heterocycles derivatives as novel antitubercular agents.
Future Medicinal Chemistry 2018 September 2
AIM: Tuberculosis (TB) is one of the world's deadliest chronic infectious diseases caused mainly by Mycobacterium tuberculosis (MTB). Many nitrofuran derivatives were found to possess promising anti-TB potential and have been widely studied. In our previous study, we discovered diazaspiro-nitrofuran IMB1701-1702 as potent anti-TB agents.
METHODOLOGY: We report herein a series of nitrofuranyl methyl N-heterocycles based on IMB1701-1702. Results reveal that most of them show potent activity (minimum inhibitory concentration: <0.016-0.062 μg/ml) against MTB H37Rv strain. Especially, compound 7h without cytotoxicity, has the same minimum inhibitory concentration value of ≤0.016 μg/ml as PBTZ169 against both MTB H37Rv strain and two clinically isolated multidrug-resistant MTB strains.
CONCLUSION: The newly designed compound 7h might be a promising anti-TB candidate.
METHODOLOGY: We report herein a series of nitrofuranyl methyl N-heterocycles based on IMB1701-1702. Results reveal that most of them show potent activity (minimum inhibitory concentration: <0.016-0.062 μg/ml) against MTB H37Rv strain. Especially, compound 7h without cytotoxicity, has the same minimum inhibitory concentration value of ≤0.016 μg/ml as PBTZ169 against both MTB H37Rv strain and two clinically isolated multidrug-resistant MTB strains.
CONCLUSION: The newly designed compound 7h might be a promising anti-TB candidate.
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