Filamenting temperature sensitive protein Z (FtsZ) is an essential bacterial cell division protein and a promising target for the development of new antibacterial therapeutics. As a part of our ongoing SAR studies on 2,5,6-trisubstituted benzimidazoles as antitubercular agents targeting Mtb-FtsZ, a new library of compounds with modifications at the 2 position was designed, synthesized and evaluated for their activity against Mtb-H37Rv. This new library of trisubstituted benzimidazoles exhibited MIC values in the range of 0.004–50 μg mL⁻¹. Compounds 6b, 6c, 20f and 20g showed excellent growth inhibitory activities ranging from 0.004–0.08 μg mL⁻¹. This SAR study has led to the discovery of a remarkably potent compound 20g (MIC 0.0039 μg mL⁻¹; normalized MIC 0.015 μg mL⁻¹). Our 3DQSAR model predicted 20g as the most potent compound in the library.

中文翻译：

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靶向 Mtb-FtsZ 的 2,5,6-三取代苯并咪唑作为抗结核药物的构效关系研究

丝状温度敏感蛋白 Z (FtsZ) 是一种必需的细菌细胞分裂蛋白，也是开发新抗菌疗法的有希望的靶点。作为我们正在进行的关于 2,5,6-三取代苯并咪唑作为靶向Mtb -FtsZ 的抗结核药物的 SAR 研究的一部分，设计、合成了一个在 2 位进行修饰的新化合物库，并评估了它们对Mtb -H37Rv的活性。这个新的三取代苯并咪唑文库的 MIC 值在 0.004–50 μg mL ^-1范围内。化合物6b、6c、20f和20g在 0.004–0.08 μg mL ^-1范围内表现出优异的生长抑制活性. 该 SAR 研究导致发现了一种非常有效的化合物20g（MIC 0.0039 μg mL ^-1；标准化 MIC 0.015 μg mL ^-1）。我们的 3DQSAR 模型预测20g是库中最有效的化合物。