期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 3, 页码 930-936出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.11.113
关键词
Glutamate racemase; Helicobacter pylori; Pyridodiazepine; MurI inhibitor
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.
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