The discovery of azepane sulfonamides as potent 11β-HSD1 inhibitors

被引：13

作者：

Neelamkavil, Santhosh F. ^{[1
]}

Boyle, Craig D. ^{[1
]}

Chackalamannil, Samuel ^{[1
]}

Greenlee, William J. ^{[1
]}

Zhang, Lili ^{[1
]}

Terracina, Giuseppe ^{[1
]}

机构：

[1] Schering Plough Corp, Res Inst, Kenilworth, NJ 07033 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 16期

关键词：

11; beta-HSD1; beta-HSD2; Diabetes; Obesity; Cortisol; Cortisone; Azepine sulfonamides; 11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE-1; OBESITY;

D O I：

10.1016/j.bmcl.2009.07.003

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Discovery of a series of azepine sulfonamides as potent inhibitors of 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1) is described. SAR studies at the 4-position of the azepane ring have resulted in the discovery of a very potent compound 30 which has an 11 beta-HSD1 IC50 of 3.0 nM. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：4563 / 4565

页数：3

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