文献类型：期刊文献

英文题名：Identification of simple arylfluorosulfates as potent agents against resistant bacteria

作者：Zhang, Jiong[1];Zhao, Xiangxiang[2];Cappiello, John R.[3];Yang, Yi[3];Cheng, Yunfei;Liu, Guang[2];Fang, Wenjing[2];Luo, Yinzhu[4];Zhang, Yu[4];Dong, Jiajia[1];Zhang, Lixin[2];Sharpless, K. Barry[3]

机构：[1]Chinese Acad Sci, Univ Chinese Acad Sci, Shanghai Inst Organ Chem, Ctr Excellence Mol Synth,Key Lab Organofluorine C, Shanghai 200032, Peoples R China;[2]East China Univ Sci & Technol, State Key Lab Bioreactor Engn, Shanghai 200237, Peoples R China;[3]Scripps Res Inst, Dept Chem, La Jolla, CA 92037 USA;[4]Guangdong Lab Anim Monitoring Inst, Guangdong Prov Key Lab Lab Animals, Guangzhou 510663, Peoples R China

年份：2021

卷号：118

期号：28

外文期刊名：PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

收录：;WOS:【SCI-EXPANDED(收录号:WOS:000685028700003)】；

基金：K.B.S., Y.Y., and J.R.C. were partially supported by the Skaggs Institute of Chemical Biology and the NIH (R01 GM117145) ; J.D. and J.Z. acknowledge the support from the National Natural Science Foundation of China (Grants NSFC 21672240 and NSFC 21421002) , the Strategic Priority Research Program of the Chinese Academy of Sciences (CAS) (Grant XDB20020300) , the Key Research Program of Frontier Sciences (CAS, Grant QYZDBSSWSLH028) , and Shanghai Science and Technology Committee (Grants 18JC1415500 and 18401933502) ; and L.Z., X.Z., G.L., W.F., Y.L., and Y.Z. were supported by the National Natural Science Foundation of China (Grant 31720103901) , the 111 Project (B18022) , the Shandong Taishan Scholar Program, and the Open Project Funding of the State Key Laboratory of Bioreactor Engineering.

语种：英文

外文关键词：SuFEx; click chemistry; antibacterial agents; multidrug resistance; biofilm disruption

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.