Adamantane sulfone and sulfonamide 11-β-HSD1 Inhibitors

被引：60

作者：

Sorensen, Bryan ^{[1
]}

Winn, Martin ^{[1
]}

Rohde, Jeff ^{[1
]}

Shuai, Qi ^{[1
]}

Wang, Jiahong ^{[1
]}

Fung, Steven ^{[1
]}

Monzon, Katina ^{[1
]}

Chiou, William ^{[1
]}

Stolarik, DeAnne ^{[1
]}

Imade, Hovis ^{[1
]}

Pan, Liping ^{[1
]}

Deng, Xiaoqing ^{[1
]}

Chovan, Linda ^{[1
]}

Longenecker, Kenton ^{[1
]}

Judge, Russell ^{[1
]}

Qin, Wenying ^{[1
]}

Brune, Michael ^{[1
]}

Camp, Heidi ^{[1
]}

Frevert, Ernst U. ^{[1
]}

Jacobson, Peer ^{[1
]}

Link, J. T. ^{[1
]}

机构：

[1] Abbott Labs, Dept 47F, Abbott Pk, IL 60064 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 02期

关键词：

11-beta-HSD-1; HSD1; 11-beta-hydroxysteroid dehydrogenase; inhibitor; adamantane; sulfone; sulfonamide;

D O I：

10.1016/j.bmcl.2006.10.008

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Potent and selective adamantane sulfone and sulfonamide inhibitors of 11-beta-HSD-1 have been discovered. Selected compounds from these series have robust pharmacokinetic profiles and strongly inhibit liver, fat, and brain HSD1 for extended periods after oral dosing. (c) 2006 Elsevier Ltd. All rights reserved.

引用

页码：527 / 532

页数：6

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