生物素蛋白连接酶抑制剂的卤化作用可提高对金黄色葡萄球菌的全细胞活性。
Halogenation of Biotin Protein Ligase Inhibitors Improves Whole Cell Activity against Staphylococcus aureus.
作者信息
Paparella Ashleigh S, Lee Kwang Jun, Hayes Andrew J, Feng Jiage, Feng Zikai, Cini Danielle, Deshmukh Sonali, Booker Grant W, Wilce Matthew C J, Polyak Steven W, Abell Andrew D
机构信息
Department of Molecular and Cellular Biology, University of Adelaide , North Tce, Adelaide, South Australia 5005, Australia.
Department of Chemistry, University of Adelaide , North Tce, Adelaide, South Australia 5005, Australia.
出版信息
ACS Infect Dis. 2018 Feb 9;4(2):175-184. doi: 10.1021/acsinfecdis.7b00134. Epub 2017 Nov 16.
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.
我们报道了5-卤代-1,2,3-三唑类化合物作为金黄色葡萄球菌生物素蛋白连接酶抑制剂的合成及评估。与非卤代类似物相比，卤代化合物展现出显著增强的抗菌活性。重要的是，5-氟-1,2,3-三唑化合物4c对金黄色葡萄球菌ATCC49775具有抗菌活性，其最低抑菌浓度（MIC）为8μg/mL。
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