Heteroaryl substituted bis-trifluoromethyl carbinols as malonyl-CoA decarboxylase inhibitors

被引：18

作者：

Cheng, Jie-Fei

Mak, Chi Ching

Huang, Yujin

Penuliar, Richard

Nishimoto, Masahiro

Zhang, Lin

Chen, Mi

Wallace, David

Arrhenius, Thomas

Chu, Donald

Yang, Guang

Barbosa, Miguel

Barr, Rick

Dyck, Jason R. B.

Lopaschuk, Gary D.

Nadzan, Alex M.

机构：

[1] Chugai Pharma LLC, Dept Chem & Discovery Biol, San Diego, CA 92121 USA

[2] Univ Alberta, Metab Modulator Res Ltd, Res Transit Facil 2020, Edmonton, AB, Canada

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 13期

关键词：

malonyl-CoA; acetyl-CoA; malonyl-CoA decarboxylase; MCD; fatty acid oxidation; glucose oxidation;

D O I：

10.1016/j.bmcl.2006.03.100

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of heteroaryl-substituted bis-trifluoromethyl carbinols were prepared and evaluated as malonyl-CoA decarboxylase (MCD) inhibitors. Some thiazole-based derivatives showed potent in vitro MCD inhibitory activities and significantly increased glucose oxidation rates in isolated working rat hearts. (c) 2006 Elsevier Ltd. All rights reserved.

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收藏

页码：3484 / 3488

页数：5

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