Bis-aryl triazoles as selective inhibitors of 11β-hydroxysteroid dehydrogenase type 1

被引：19

作者：

Aster, Susan D. ^{[1
]}

Graham, Donald W. ^{[1
]}

Kharbanda, Divya ^{[1
]}

Patel, Gool ^{[1
]}

Ponpipom, Mitree ^{[1
]}

Santorelli, Gina M. ^{[1
]}

Szymonifka, Michael J. ^{[1
]}

Mundt, Steven S. ^{[2
]}

Shah, Kashmira ^{[2
]}

Springer, Marty S. ^{[2
]}

Thieringer, Rolf ^{[2
]}

Hermanowski-Vosatka, Anne ^{[2
]}

Wright, Samuel D. ^{[2
]}

Xiao, Jianying ^{[2
]}

Zokian, Hratch ^{[2
]}

Balkovec, James M. ^{[1
]}

机构：

[1] Merck & Co Inc, Dept Med Chem, Rahway, NJ 07065 USA

[2] Merck & Co Inc, Dept Cardiovasc Dis, Rahway, NJ 07065 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 09期

关键词：

11 beta-hydroxysteroid dehydrogenase; metabolic syndrome; bis-aryl triazoles;

D O I：

10.1016/j.bmcl.2008.04.010

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

3-Aryl-5-phenyl-(1,2,4)-triazoles were identified as selective inhibitors of 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1). They are active in both in vitro and an in vivo mouse pharmacodynamic (PD) model. The synthesis and structure activity relationships are presented. (c) 2008 Elsevier Ltd. All rights reserved.

引用

页码：2799 / 2804

页数：6

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