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作为抗结核药物先导的必需分枝杆菌细胞壁脂肪酶（Rv3802c）抑制剂。

Inhibitors of an essential mycobacterial cell wall lipase (Rv3802c) as tuberculosis drug leads.

机构信息

Centenary Institute of Cancer Medicine and Cell Biology, Newtown, NSW 2042, Australia.

出版信息

Chem Commun (Camb). 2011 May 14;47(18):5166-8. doi: 10.1039/c0cc05635a. Epub 2011 Mar 7.

DOI:10.1039/c0cc05635a
PMID:21384024
Abstract

The first targeted inhibitors of an essential M. tuberculosis cell wall lipase, Rv3802c, are described. Lead compounds exhibited nanomolar inhibition of the enzyme, and encouraging antibacterial activity against M. tuberculosis in vitro, supporting Rv3802c as a novel TB drug target.

摘要

首次描述了结核分枝杆菌必需的细胞壁脂肪酶 Rv3802c 的靶向抑制剂。先导化合物对该酶表现出纳摩尔级的抑制作用，并在体外对结核分枝杆菌表现出令人鼓舞的抗菌活性，这支持 Rv3802c 作为一种新的结核病药物靶点。

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