探索9-苄基嘌呤作为革兰氏阳性菌中谷氨酸消旋酶（MurI）抑制剂的研究。
Exploring 9-benzyl purines as inhibitors of glutamate racemase (MurI) in Gram-positive bacteria.
作者信息
Geng Bolin, Breault Gloria, Comita-Prevoir Janelle, Petrichko Randy, Eyermann Charles, Lundqvist Tomas, Doig Peter, Gorseth Elise, Noonan Brian
机构信息
AstraZeneca R&D Boston, Infection Discovery, 35 Gatehouse Drive, Waltham, MA 02451, USA.
出版信息
Bioorg Med Chem Lett. 2008 Aug 1;18(15):4368-72. doi: 10.1016/j.bmcl.2008.06.068. Epub 2008 Jun 24.
PMID:18614367
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.
摘要
对一系列筛选命中化合物进行的早期SAR研究产生了一系列9-苄基嘌呤，作为细菌谷氨酸消旋酶（MurI）的抑制剂，具有微摩尔级的酶活性和改善的物理性质。获得了X射线共晶体EI结构。
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