Discovery and SAR development of thienopyridones: A class of small molecule AMPK activators

被引：39

作者：

Zhao, Gang ^{[1
]}

Iyengar, Rajesh R. ^{[1
]}

Judd, Andrew S. ^{[1
]}

Cool, Barbara ^{[1
]}

Chiou, William ^{[1
]}

Kifle, Lemma ^{[1
]}

Frevert, Ernst ^{[1
]}

Sham, Hing ^{[1
]}

Kym, Philip R. ^{[1
]}

机构：

[1] Abbott Labs, Metab Dis Res, Abbott Pk, IL 60064 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 12期

关键词：

AMPK; obesity; diabetes;

D O I：

10.1016/j.bmcl.2007.04.011

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

AMP-activated protein kinase (AMPK) is well established as a sensor and regulator of intracellular and whole-body energy metabolism. A high-throughput screen was performed in order to identify chemotypes that are bound by AMPK. A novel thienopyridone compound (1) was identified and subsequently optimized. The structure-activity relationships that emerged from this effort are described. (c) 2007 Elsevier Ltd. All rights reserved.

引用

页码：3254 / 3257

页数：4

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