新型强效 DNA 拓扑异构酶抑制剂的合成、结构与抗菌活性：N’-苯甲酰基-3-(4-溴苯基)-1H-吡唑-5-甲酰肼衍生物。
Synthesis, structure and antibacterial activity of potent DNA gyrase inhibitors: N'-benzoyl-3-(4-bromophenyl)-1H-pyrazole-5-carbohydrazide derivatives.
机构信息
State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing, China.
出版信息
PLoS One. 2013 Jul 29;8(7):e69751. doi: 10.1371/journal.pone.0069751. Print 2013.
A total of 19 novel (3a-3s) N'-benzoyl-3-(4-bromophenyl)-1H-pyrazole-5-carbohydrazide analogs were designed, synthesized, and evaluated for biological activities as potential DNA gyrase inhibitors. The results showed that compound 3k can strongly inhibit Staphylococcus aureus DNA gyrase and Bacillus subtilis DNA gyrase (with IC50 of 0.15 µg/mL and 0.25 µg/mL, respectively). Structure-activity relationships were also discussed base on the biological and docking simulation results.
总共设计、合成了 19 种新型（3a-3s）N'-苯甲酰基-3-(4-溴苯基)-1H-吡唑-5-甲酰肼类似物，并评估了它们作为潜在 DNA 拓扑异构酶抑制剂的生物活性。结果表明，化合物 3k 能强烈抑制金黄色葡萄球菌 DNA 拓扑异构酶和枯草芽孢杆菌 DNA 拓扑异构酶（IC50 分别为 0.15 µg/mL 和 0.25 µg/mL）。基于生物和对接模拟结果，还讨论了构效关系。
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