合成和评价硝基呋喃甲基 N-杂环衍生物作为新型抗结核药物。
Synthesis and evaluation of nitrofuranyl methyl N-heterocycles derivatives as novel antitubercular agents.
机构信息
Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, PR China.
College of Chemistry & Material Science, Hebei Normal University, Hebei Shijiazhuang 050024, PR China.
出版信息
Future Med Chem. 2018 Sep 1;10(17):2059-2068. doi: 10.4155/fmc-2018-0112. Epub 2018 Jul 11.
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.
目的
结核病（TB）是由结核分枝杆菌（MTB）引起的全球最致命的慢性传染病之一。许多硝呋类衍生物被发现具有有希望的抗结核潜力，并得到了广泛研究。在我们之前的研究中，我们发现二氮杂螺-硝呋类 IMB1701-1702 是有效的抗结核药物。
方法
我们在此报告了一系列基于 IMB1701-1702 的硝呋烷基 N-杂环化合物。结果表明，它们中的大多数对 MTB H37Rv 株具有很强的活性（最低抑菌浓度：<0.016-0.062μg/ml）。特别是化合物 7h 无细胞毒性，对 MTB H37Rv 株和两种临床分离的耐多药 MTB 株的最低抑菌浓度值与 PBTZ169 相同，均为≤0.016μg/ml。
结论
新设计的化合物 7h 可能是一种有前途的抗结核候选药物。
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