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DOI	10.1073/PNAS.2103513118
	Identification of simple arylfluorosulfates as potent agents against resistant bacteria
	Zhang J.; Zhaob X.; Cappiello J.R.; Yang Y.; Cheng Y.; Liu G.; Fang W.; Luo Y.; Zhang Y.; Dong J.; Zhang L.; Sharpless K.B.
发表日期	2021
ISSN	0027-8424
卷号	118 期号:28
英文摘要	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. © 2021 National Academy of Sciences. All rights reserved.
英文关键词	Antibacterial agents; Biofilm disruption; Click chemistry; Multidrug resistance; SuFEx
语种	英语
scopus关键词	antiinfective agent; arylfluorosulfate; gentamicin; streptomycin; unclassified drug; vancomycin; Article; Bacillus subtilis; bacterial strain; bactericidal activity; bacterium; bacterium isolate; biofilm; controlled study; Enterococcus faecium; Escherichia coli; in vitro study; Klebsiella pneumoniae; minimum inhibitory concentration; multidrug resistance; nonhuman; phenotype; Staphylococcus aureus; Staphylococcus epidermidis; structure activity relation; synergistic effect
来源期刊	Proceedings of the National Academy of Sciences of the United States of America
文献类型	期刊论文
条目标识符	http://gcip.llas.ac.cn/handle/2XKMVOVA/238866
作者单位	Key Laboratory of Organofluorine Chemistry, Center for Excellence in Molecular Synthesis, Shanghai Institute of Organic Chemistry, University of the Chinese Academy of Sciences, Chinese Academy of Sciences, Shanghai, 200032, China; State Key Laboratory of Bioreactor Engineering, East China University of Science and Technology, Shanghai, 200237, China; Department of Chemistry, The Scripps Research Institute, San diego, CA 92037, United States; Guangdong Provincial Key Laboratory of Laboratory Animals, Guangdong Laboratory Animals Monitoring Institute, Guangzhou, 510663, China
推荐引用方式 GB/T 7714	Zhang J.,Zhaob X.,Cappiello J.R.,et al. Identification of simple arylfluorosulfates as potent agents against resistant bacteria[J],2021,118(28).
APA	Zhang J..,Zhaob X..,Cappiello J.R..,Yang Y..,Cheng Y..,...&Sharpless K.B..(2021).Identification of simple arylfluorosulfates as potent agents against resistant bacteria.Proceedings of the National Academy of Sciences of the United States of America,118(28).
MLA	Zhang J.,et al."Identification of simple arylfluorosulfates as potent agents against resistant bacteria".Proceedings of the National Academy of Sciences of the United States of America 118.28(2021).