效力
链霉素
生物膜
微生物学
庆大霉素
细菌
化学
多重耐药
生物
秀丽隐杆线虫
抗药性
抗生素
体外
生物化学
遗传学
基因
作者
Jiong Zhang,Xiangxiang Zhao,John Cappiello,Yi Yang,Yunfei Cheng,Liu Guang,Wenjing Fang,Yinzhu Luo,Yu Zhang,Jiajia Dong,Lixin Zhang,K. Barry Sharpless
标识
DOI:10.1073/pnas.2103513118
摘要
Sulfur fluoride exchange (SuFEx), a next generation of click chemistry, opens an avenue for drug discovery. We report here the discovery and structure-activity relationship studies of a series of arylfluorosulfates, synthesized via SuFEx, as antibacterial agents. Arylfluorosulfates 3, 81, and 101 showed potency to overcome multidrug resistance and were not susceptible to the generation of resistance. They exhibited rapid bactericidal potency and selectively killed gram-positive bacterial strains. These compounds also exhibited the ability to disrupt established bacterial biofilm and kill persisters derived from biofilm. Furthermore, arylfluorosulfate 3 had a synergistic effect with streptomycin and gentamicin. In addition, their anti-MRSA potency was evaluated and determined by the Caenorhabditis elegans model.
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