Potent and selective inhibitors of Helicobacter pylori glutamate racemase (MurI): Pyridodiazepine amines
Potent and selective inhibitors of Helicobacter pylori glutamate racemase (MurI): Pyridodiazepine amines
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DOI：
10.1016/j.bmcl.2008.11.113
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发表时间：
2009-02-01
影响因子：
2.7
通讯作者：
Lundqvist, Tomas
中科院分区：
文献类型：
--
作者：
Geng, Bolin;Basarab, Gregory;Lundqvist, Tomas
HTS筛选命中的SAR研究产生了一系列吡啶并二氮杂卓胺作为幽门螺杆菌谷氨酸消旋酶（MurI）的强效抑制剂，显示出高度选择性的抗H。幽门螺杆菌活性，显著改善的溶解度和降低的血浆蛋白结合。获得了X射线共晶E-I结构。这些非竞争性抑制剂结合在MurI二聚体界面。(C)2008爱思唯尔有限公司保留所有权利。
An SAR study of an HTS screening hit generated a series of pyridodiazepine amines as potent inhibitors of Helicobacter pylori glutamate racemase (MurI) showing highly selective anti-H. pylori activity, marked improved solubility, and reduced plasma protein binding. X-ray co-crystal E-I structures were obtained. These uncompetitive inhibitors bind at the MurI dimer interface. (C) 2008 Elsevier Ltd. All rights reserved.