Phenylacetic acid derivatives as hPPAR Agonists

被引：36

作者：

Santini, C

Berger, GD

Han, W

Mosley, R

MacNaul, K

Berger, J

Doebber, T

Wu, M

Moller, DE

Tolman, RL

Sahoo, SP

机构：

[1] Merck Res Labs, Dept Basic Chem, Rahway, NJ 07065 USA

[2] Merck Res Labs, Dept Mol Endocrinol, Rahway, NJ 07065 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 07期

关键词：

D O I：

10.1016/S0960-894X(03)00115-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Beginning with the weakly active lead structure 1, a new series of WAR agonists was developed. In vivo glucose and triglyceride lowering activity was obtained by homologation and oxamination to 3, then conversion to substituted benzisoxazoles 4 and 5. Further manipulation afforded benzofurans 6 and 7. Compound 7 was of comparable potency as a glucose and triglyceride lowering agent in insulin resistant rodents to BRL 49653. (C) 2003 Elsevier Science Ltd. All rights reserved.

引用

页码：1277 / 1280

页数：4

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