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

被引：17

作者：

Clark, Richard F. ^{[1
]}

Zhang, Tianyuan ^{[1
]}

Xin, Zhili ^{[1
]}

Liu, Gang ^{[1
]}

Wang, Ying ^{[1
]}

Hansen, T. Matthew ^{[1
]}

Wang, Xiaojun ^{[1
]}

Wang, Rongqi ^{[1
]}

Zhang, Xiaolin ^{[1
]}

Frevert, Ernst U. ^{[1
]}

Camp, Heidi S. ^{[1
]}

Beutel, Bruce A. ^{[1
]}

Sham, Hing L. ^{[1
]}

Gu, Yu i Gu ^{[1
]}

机构：

[1] Abbott Labs, Abbott Pk, IL 60064 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 23期

关键词：

acetyl-CoA carboxylase; insulin resistance; obesity; type; 2; diabetes; FATTY-ACID OXIDATION; MUTANT MICE; METABOLISM; OBESITY; TISSUE;

D O I：

10.1016/j.bmcl.2006.08.100

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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. (c) 2006 Elsevier Ltd. All rights reserved.

引用

收藏

页码：6078 / 6081

页数：4

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