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Bioorg Med Chem Lett. 2009 Feb 1;19(3):930-6. doi: 10.1016/j.bmcl.2008.11.113. Epub 2008 Dec 6.

Potent and selective inhibitors of Helicobacter pylori glutamate racemase (MurI): pyridodiazepine amines.

Author information

1
AstraZeneca R&D Boston, Infection Discovery, 35 Gatehouse Drive, Waltham, MA 02451, USA. bolin.geng@astrazeneca.com

Abstract

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.

PMID:
19097892
DOI:
10.1016/j.bmcl.2008.11.113
[Indexed for MEDLINE]

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