Discovery of new Gram-negative antivirulence drugs:: Structure and properties of novel E-coli WaaC inhibitors
Discovery of new Gram-negative antivirulence drugs:: Structure and properties of novel E-coli WaaC inhibitors
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DOI：
10.1016/j.bmcl.2008.05.117
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发表时间：
2008-07-15
影响因子：
2.7
通讯作者：
Aschenbrenner, A.
中科院分区：
文献类型：
--
作者：
Moreau, F.;Desroy, N.;Aschenbrenner, A.
庚糖基转移酶，如WaaC代表有前途的和有吸引力的目标，发现新的革兰氏阴性抗菌药物的基础上的抗毒力机制。我们在此报告我们的方法来识别的第一微摩尔抑制剂WaaC和初步的SAR产生的2-芳基-5-甲基-4-（5-芳基-呋喃-2-基-亚甲基）-2，4-二氢-吡唑-3-酮，通过虚拟筛选确定了这个家庭。(c)2008爱思唯尔有限公司保留所有权利。
Heptosyltransferases such as WaaC represent promising and attractive targets for the discovery of new Gram-negative antibacterial drugs based on antivirulence mechanisms. We report herein our approach to the identification of the first micromolar inhibitors of WaaC and the preliminary SAR generated from this family of 2-aryl-5-methyl-4-(5-aryl-furan-2-yl-methylene)-2,4-dihydro-pyrazol-3-ones identified by virtual screening. (c) 2008 Elsevier Ltd. All rights reserved.