2-Hydroxy-N-arylbenzenesulfonamides as ATP-citrate lyase inhibitors

被引：70

作者：

Li, James J.

Wang, Haixia

Tino, Joseph A.

Robl, Jeffrey A.

Herpin, Timothy F.

Lawrence, R. Michael

Biller, Scott

Jamil, Haris

Ponticiello, Randy

Chen, Luping

Chu, Ching-hsuen

Flynn, Neil

Cheng, Dong

Zhao, Rulin

Chen, Bangchi

Schnur, Dora

Obermeier, Mary T.

Sasseville, Vito

Padmanabha, Ramesh

Pike, Kristen

Harrity, Thomas

机构：

[1] Bristol Myers Squibb Pharmaceut Res Inst, Princeton, NJ 08543 USA

[2] Bristol Myers Squibb Co, Pharmaceut Res Inst, Wallingford, CT 06492 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 11期

关键词：

ATP-citrate lyase (ACL) inhibitors; lipid; glycemic profiles and weight loss;

D O I：

10.1016/j.bmcl.2007.03.017

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A novel series of 2-hydroxy-N-arylbenzenesulfonamides were identified to be ATP-citrate lyase (ACL) inhibitors with compound 9 displaying potent in vitro activity (IC50 = 0.13 mu M). Chronic oral dosing of compound 9 in high-fat fed mice lowered plasma cholesterol, triglyceride, and glucose, as well as inhibited weight gain. (C) 2007 Elsevier Ltd. All rights reserved.

引用

收藏

页码：3208 / 3211

页数：4

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