We report the synthesis and evaluation of 5-halogenated-1,2,3-triazoles as inhibitors of biotin protein ligase from Staphylococcus aureus. The halogenated compounds exhibit significantly improved antibacterial activity over their nonhalogenated counterparts. Importantly, the 5-fluoro-1,2,3-triazole compound 4c displays antibacterial activity against S. aureus ATCC49775 with a minimum inhibitory concentration (MIC) of 8 μg/mL.

中文翻译：

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生物素蛋白连接酶抑制剂的卤化提高了针对金黄色葡萄球菌的全细胞活性

我们报告了5-卤代1,2,3-三唑作为金黄色葡萄球菌生物素蛋白连接酶抑制剂的合成和评价。卤代化合物显示出比其非卤代对应物显着改善的抗菌活性。重要的是，5-氟-1,2,3-三唑化合物4c对金黄色葡萄球菌ATCC49775表现出抗菌活性，最低抑菌浓度（MIC）为8μg/ mL。