CoA adducts of 4-oxo-4-phenylbut-2-enoates: inhibitors of MenB from the M. tuberculosis menaquinone biosynthesis pathway

…, SE Knudson, HJ Li, CT Lai, C Simmerling…

文献索引：Li, Xiaokai; Liu, Nina; Zhang, Huaning; Knudson, Susan E.; Li, Huei-Jiun; Lai, Cheng-Tsung; Simmerling, Carlos; Slayden, Richard A.; Tonge, Peter J. ACS Medicinal Chemistry Letters, 2011 , vol. 2, # 11 p. 818 - 823

全文：HTML全文

被引用次数: 18

摘要

A high-throughput screen led to the discovery of 2-amino-4-oxo-4-phenylbutanoate inhibitors of the 1, 4-dihydroxy-2-naphthoyl-CoA synthase (MenB) from the menaquinone biosynthesis pathway in Mycobacterium tuberculosis. However, these compounds are unstable in solution and eliminate to form the corresponding 4-oxo-4-phenylbut-2-enoates that then react with CoA in situ to form nanomolar inhibitors of MenB. The potency of these ...