Potent and selective inhibitors of Helicobacter pylori glutamate racemase (MurI): pyridodiazepine amines.
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Geng B, Basarab G, Comita-Prevoir J, Gowravaram M, Hill P, Kiely A, Loch J, MacPherson L, Morningstar M, Mullen G, Osimboni E, Satz A, Eyermann C, Lundqvist T
Potent and selective inhibitors of Helicobacter pylori glutamate racemase (MurI): pyridodiazepine amines.
Bioorg Med Chem Lett. 2009 Feb 1;19(3):930-6. doi: 10.1016/j.bmcl.2008.11.113. Epub 2008 Dec 6.
- PubMed ID
- 19097892 [ View in PubMed]
- 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.