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

Bioorg Med Chem Lett

Authors	Bolin Geng Gregory Basarab Janelle Comita-Prevoir Madhusudhan Gowravaram Pamela Hill Andrew Kiely James Loch Lawrence MacPherson Marshall Morningstar George Mullen Ekundayo Osimboni Alexander Satz Charles Eyermann Tomas Lundqvist
Keywords	Animals Humans Mice Anti-Infective Agents Drug Design Amines Chemistry, Pharmaceutical Structure-Activity Relationship Dimerization Binding, Competitive Molecular Conformation Amino Acid Isomerases Helicobacter Infections Helicobacter pylori Inhibitory Concentration 50
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.
Year of Publication	2009
Journal	Bioorg Med Chem Lett
Volume	19
Issue	3
Pages	930-6
Date Published	2009 Feb 01
ISSN	1464-3405
DOI	10.1016/j.bmcl.2008.11.113
PubMed ID	19097892
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