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新型噻唑基苯基醚衍生物系列的构效关系，该系列衍生物具有强效和选择性乙酰辅酶A羧化酶2抑制活性。

Structure-activity relationships for a novel series of thiazolyl phenyl ether derivatives exhibiting potent and selective acetyl-CoA carboxylase 2 inhibitory activity.

作者信息

Clark Richard F, Zhang Tianyuan, Xin Zhili, Liu Gang, Wang Ying, Hansen T Matthew, Wang Xiaojun, Wang Rongqi, Zhang Xiaolin, Frevert Ernst U, Camp Heidi S, Beutel Bruce A, Sham Hing L, Gu Yu Gui

机构信息

Metabolic Disease Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, IL 60064, USA.

出版信息

Bioorg Med Chem Lett. 2006 Dec 1;16(23):6078-81. doi: 10.1016/j.bmcl.2006.08.100. Epub 2006 Sep 14.

DOI:10.1016/j.bmcl.2006.08.100
PMID:16973360
Abstract

Structure-activity relationships for a recently discovered thiazolyl phenyl ether series of acetyl-CoA carboxylase (ACC) inhibitors were investigated. Preliminary efforts to optimize the series through modification of the distal aryl ether moiety of the lead scaffold resulted in the identification of compounds exhibiting low-nanomolar potency and isozyme-selective ACC2 activity.

摘要

对最近发现的噻唑基苯基醚系列乙酰辅酶A羧化酶（ACC）抑制剂的构效关系进行了研究。通过修饰先导骨架的远端芳基醚部分来优化该系列的初步努力，导致鉴定出具有低纳摩尔效力和同工酶选择性ACC2活性的化合物。

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