探索8-苄基蝶啶-6,7-二酮作为革兰氏阳性菌中谷氨酸消旋酶（MurI）的抑制剂。
Exploring 8-benzyl pteridine-6,7-diones as inhibitors of glutamate racemase (MurI) in gram-positive bacteria.
作者信息
Breault Gloria A, Comita-Prevoir Janelle, Eyermann Charles J, Geng Bolin, Petrichko Randy, Doig Peter, Gorseth Elise, Noonan Brian
机构信息
Infection Discovery, AstraZeneca R&D Boston, 35 Gatehouse Drive, Waltham, MA 02451, USA.
出版信息
Bioorg Med Chem Lett. 2008 Dec 1;18(23):6100-3. doi: 10.1016/j.bmcl.2008.10.022. Epub 2008 Oct 8.
PMID:18947997
Abstract
A successful scaffold-hopping approach gave a novel series of inhibitors of bacterial glutamate racemase (MurI). Early SAR studies of the 8-benzyl pteridine-6,7-diones led to compounds with micromolar enzyme potency and antibacterial activity.
摘要
一种成功的骨架跃迁方法产生了一系列新型的细菌谷氨酸消旋酶（MurI）抑制剂。对8-苄基蝶啶-6,7-二酮的早期构效关系研究得到了具有微摩尔级酶活性和抗菌活性的化合物。
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