Discovery of piperidine-aryl urea-based stearoyl-CoA desaturase 1 inhibitors

被引：68

作者：

Xin, Zhili ^{[1
]}

Zhao, Hongyu ^{[1
]}

Serby, Michael D. ^{[1
]}

Liu, Bo ^{[1
]}

Liu, Mei ^{[1
]}

Szczepankiewicz, Bruce G. ^{[1
]}

Nelson, Lissa T. J. ^{[1
]}

Smith, Harriet T. ^{[1
]}

Suhar, Tom S. ^{[1
]}

Janis, Rich S. ^{[1
]}

Cao, Ning ^{[1
]}

Camp, Heidi S. ^{[1
]}

Collins, Christine A. ^{[1
]}

Sham, Hing L. ^{[1
]}

Surowy, Teresa K. ^{[1
]}

Liu, Gang ^{[1
]}

机构：

[1] Abbott Labs, Global Pharmaceut Res & Dev, Abbott Pk, IL 60064 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 15期

关键词：

SCD1; inhibitors; desaturation index;

D O I：

10.1016/j.bmcl.2008.06.088

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of structurally novel stearoyl-CoA desaturase1 (SCD1) inhibitors has been identified via molecular scaffold manipulation. Preliminary structure-activity relationship (SAR) studies led to the discovery of potent, and orally bioavailable piperidine-aryl urea-based SCD1 inhibitors. 4-(2-Chlorophenoxy)-N-[3-(methyl carbamoyl)phenyl]piperidine-1-carboxamide 4c exhibited robust in vivo activity with dose-dependent desaturation index lowering effects. (c) 2008 Elsevier Ltd. All rights reserved.

引用

页码：4298 / 4302

页数：5

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