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苯并咪唑衍生物的设计与合成及其抗分枝杆菌活性

Design and synthesis of benzimidazole derivatives as antimycobacterial agents.

机构信息

Department of Chemistry, University of Delhi, New Delhi, India.

Tuberculosis Research Laboratory, Translational Health Science and Technology Institute, Faridabad, Haryana, India.

出版信息

J Biochem Mol Toxicol. 2022 Sep;36(9):e23123. doi: 10.1002/jbt.23123. Epub 2022 Jun 10.

DOI:10.1002/jbt.23123
PMID:35686933
Abstract

A series of 2,5-disubstituted benzimidazole derivatives was synthesized with the aim to identify compounds with potent anti-TB activity. All the compounds were screened in vitro against cultured Mycobacterium tuberculosis H Rv strain and found to be exhibiting MIC values in the range of 0.195-100 µM. Out of 43 synthesized compounds, two compounds 11h and 13e showed better anti-TB activity than the reference drug isoniazid.

摘要

我们合成了一系列 2,5-二取代苯并咪唑衍生物,旨在寻找具有高效抗结核活性的化合物。所有化合物均在体外对培养的结核分枝杆菌 H37Rv 株进行了筛选,结果显示其 MIC 值在 0.195-100 μM 范围内。在所合成的 43 种化合物中,化合物 11h 和 13e 的抗结核活性优于对照药物异烟肼。

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