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Exploring 9-benzyl purines as inhibitors of glutamate racemase (MurI) in Gram-positive bacteria |
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| Authors: | Geng Bolin Breault Gloria Comita-Prevoir Janelle Petrichko Randy Eyermann Charles Lundqvist Tomas Doig Peter Gorseth Elise Noonan Brian |
| Institution: | aAstraZeneca R&D Boston, Infection Discovery, 35 Gatehouse Drive, Waltham, MA 02451, USA;bAstraZeneca R&D Mölndal, Global Structural Chemistry, Mölndal, SE-43183, Sweden |
| Abstract: | An early SAR study of a screening hit series has generated a series of 9-benzyl purines as inhibitors of bacterial glutamate racemase (MurI) with micromolar enzyme potency and improved physical properties. X-ray co-crystal EI structures were obtained. |
| Keywords: | Glutamate racemase MurI inhibitor Benzyl purine |
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