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寡氯苯是炭疽杆菌的有效抑制剂。

Oligochlorophens are potent inhibitors of Bacillus anthracis.

机构信息

Department of Biochemistry, University of Wisconsin-Madison, Madison, WI 53706-1544, USA.

出版信息

Antimicrob Agents Chemother. 2010 Sep;54(9):3988-90. doi: 10.1128/AAC.00067-10. Epub 2010 Jun 21.

DOI:10.1128/AAC.00067-10
PMID:20566769
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC2934962/
Abstract

Bacterial cytoskeletal proteins are an emerging set of targets for antibiotic development. This paper describes oligochlorophen analogs based on the monomer 4-chloro-2,6-dimethylphenol as antimicrobial agents against Bacillus anthracis. The most potent analogs have a MIC of 160 to 320 nM against B. anthracis and may target the cytoskeletal protein FtsZ. B. anthracis develops resistance to the oligochlorophens at a rate of 4.34 x 10(-10) per generation, which is approximately 10-fold lower than that of commercial antibiotics used to treat this human pathogen.

摘要

细菌细胞骨架蛋白是一组新兴的抗生素开发靶点。本文描述了基于单体 4-氯-2,6-二甲基苯酚的寡氯苯类似物,作为抗炭疽芽孢杆菌的抗菌剂。最有效的类似物对炭疽芽孢杆菌的 MIC 为 160 至 320 nM,可能针对细胞骨架蛋白 FtsZ。炭疽芽孢杆菌对寡氯苯的耐药性产生速度为每代 4.34 x 10(-10),比用于治疗这种人类病原体的商业抗生素低约 10 倍。

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本文引用的文献

1
Fluctuation analysis CalculatOR: a web tool for the determination of mutation rate using Luria-Delbruck fluctuation analysis.波动分析计算器:一种使用卢里亚-德尔布吕克波动分析来确定突变率的网络工具。
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An inhibitor of FtsZ with potent and selective anti-staphylococcal activity.一种具有强效和选择性抗葡萄球菌活性的FtsZ抑制剂。
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Cell-division inhibitors: new insights for future antibiotics.细胞分裂抑制剂:未来抗生素的新见解。
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Cytoskeletal elements in bacteria.细菌中的细胞骨架成分。
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Mutations of Bacteria from Virus Sensitivity to Virus Resistance.细菌从对病毒敏感到对病毒抗性的突变。
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Dynamic filaments of the bacterial cytoskeleton.细菌细胞骨架的动态细丝。
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8
MICs of selected antibiotics for Bacillus anthracis, Bacillus cereus, Bacillus thuringiensis, and Bacillus mycoides from a range of clinical and environmental sources as determined by the Etest.采用Etest法测定来自一系列临床和环境来源的炭疽芽孢杆菌、蜡样芽孢杆菌、苏云金芽孢杆菌和蕈状芽孢杆菌对选定抗生素的最低抑菌浓度。
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9
Targeting cell division: small-molecule inhibitors of FtsZ GTPase perturb cytokinetic ring assembly and induce bacterial lethality.靶向细胞分裂:FtsZ GTP酶的小分子抑制剂扰乱细胞分裂环组装并诱导细菌死亡。
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