A series of isopropanol-bridged carbazole azoles as potential antimicrobial agents were designed and synthesized from commercial carbazoles. Bioassay revealed that 3,6-dichlorocarbazolyl triazole 3f could effectively inhibit the growth of E. faecalis with minimal inhibitory concentration of 2 μg/mL. The active molecule 3f showed lower propensity to trigger the development of resistance in bacteria than norfloxacin and exerted rapidly bactericidal ability. Compound 3f also exhibited low cytotoxicity to normal mammalian RAW264.7 cells. Further mechanism exploration indicated that conjugate 3f was membrane active against E. faecalis and could form 3f-DNA complex by intercalating into DNA of resistant E. faecalis, which might be responsible for its antimicrobial action. Molecular docking showed an efficient binding of triazole derivative 3f with DNA gyrase enzyme through noncovalent interactions.

中文翻译：

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潜在的抗菌素与异丙醇结合的咔唑唑作为粪肠球菌的双重靶向抑制剂。

从商业咔唑中设计并合成了一系列异丙醇桥联咔唑唑作为潜在的抗菌剂。生物测定表明，3,6-二氯咔唑三唑3f可以有效抑制粪肠球菌的生长，最低抑菌浓度为2μg/ mL。活性分子3f显示出比诺氟沙星更低的引发细菌耐药性的倾向，并具有快速的杀菌能力。化合物3f对正常的哺乳动物RAW264.7细胞也显示出低细胞毒性。进一步的机理研究表明，缀合物3f对屎肠球菌具有膜活性，并且可以通过插入耐药性屎肠球菌的DNA中而形成3f-DNA复合物，这可能是其抗菌作用的原因。