Discovery and biological evaluation of adamantyl amide 11β-HSD1 inhibitors

被引：46
|
作者：
Webster, Scott P.
Ward, Peter
Binnie, Margaret
Craigie, Eilidh
McConnell, Kirsty M. M.
Sooy, Karen
Vinter, Andy
Seckl, Jonathan R.
Walker, Brian R.
机构：
[1] Univ Edinburgh, Queens Med Res Inst, Ctr Cardiovasc Sci, Endocrinol Unit, Edinburgh EH16 4TJ, Midlothian, Scotland
[2] Cresset Biomol Discovery Ltd, Letchworth SG6 4ET, Herts, England
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 10期
基金：
英国惠康基金;
关键词：
metabolic syndrome; 11; beta-HSD1; beta-HSD2; inhibitor; adamantane; amide; diabetes; 11 beta-hydroxysteroid dehydrogenase; enzyme inhibition; HSD1;
D O I：
10.1016/j.bmcl.2007.02.057
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of adamantyl amide 11 beta-HSD1 inhibitors has been discovered and chemically modified. Selected compounds are selective for 11 beta-HSD1 over 11 beta-HSD2 and possess excellent cellular potency in human and murine 11 beta-HSD1 assays. Good pharmacodynamic characteristics are observed in ex vivo assays. (c) 2007 Elsevier Ltd. All rights reserved.
引用
收藏
页码：2838 / 2843
页数：6
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