Derivatives of 8-hydroxyquinoline-antibacterial agents that target intra- and extracellular Gram-negative pathogens
Derivatives of 8-hydroxyquinoline-antibacterial agents that target intra- and extracellular Gram-negative pathogens
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DOI：
10.1016/j.bmcl.2012.03.096
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发表时间：
2012-05-15
影响因子：
2.7
通讯作者：
Elofsson, Mikael
中科院分区：
文献类型：
--
作者：
Enquist, Per-Anders;Gylfe, Asa;Elofsson, Mikael
小分子筛选鉴定出5-硝基-7-（（4-苯基哌嗪-1-基-）甲基）喹啉-8-醇INP 1750为革兰氏阴性病原体假结核耶尔森氏菌中III型分泌（T3 S）的推定抑制剂。在这项研究中，我们报告了抑制T3 S的构效关系，并表明最有效的化合物靶向细胞外细菌Y。假结核和细胞内病原体沙眼衣原体在基于细胞的感染模型。(C)2012爱思唯尔有限公司保留所有权利。
Small molecule screening identified 5-nitro-7-((4-phenylpiperazine-1-yl-)methyl)quinolin-8-ol INP1750 as a putative inhibitor of type III secretion (T3S) in the Gram-negative pathogen Yersinia pseudotuberculosis. In this study we report structure-activity relationships for inhibition of T3S and show that the most potent compounds target both the extracellular bacterium Y. pseudotuberculosis and the intracellular pathogen Chlamydia trachomatis in cell-based infection models. (C) 2012 Elsevier Ltd. All rights reserved.