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.
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收藏
页码：4563 / 4565
页数：3
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