Synthesis and Biological Evaluation of Cyclic Sulfamide Derivatives as 11β-Hydroxysteroid Dehydrogenase 1 Inhibitors

被引：18

作者：

Kim, Se Hoan ^{[1
,2
]}

Bok, Ju Han ^{[1
]}

Lee, Jae Hong ^{[1
,2
]}

Kim, Il Hyang ^{[1
,2
]}

Kwon, Sung Wook ^{[1
,2
]}

Lee, Gui Bin ^{[1
]}

Kang, Seung Kyu ^{[1
]}

Park, Ji Seon ^{[1
]}

Jung, Won Hoon ^{[1
]}

Kim, Hee Yeon ^{[1
]}

Rhee, Sang Dal ^{[1
]}

Ahn, Sung Hoon ^{[1
]}

Bae, Myung Ae ^{[1
]}

Ha, Deok Chan ^{[2
]}

Kim, Ki Young ^{[1
]}

Ahn, Jin Hee ^{[1
]}

机构：

[1] Korea Res Inst Chem Technol, Bioorgan Sci Div, Taejon 305600, South Korea

[2] Korea Univ, Dept Chem, Seoul 136701, South Korea

来源：

ACS MEDICINAL CHEMISTRY LETTERS | 2012年 / 3卷 / 02期

关键词：

diabetes; antidiabetic agents; 11 beta-hydroxysteroid dehydrogenase type 1; cyclic sulfamide; adamantyl group; 11-BETA-HSD1; INHIBITORS; METABOLIC SYNDROME; VISCERAL OBESITY; TYPE-1; MICE; HYPERGLYCEMIA;

D O I：

10.1021/ml200226x

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A new series of cyclic sulfamide derivatives were synthesized and evaluated for their ability to inhibit 11 beta-HSD1. Among this series, 18e showed good in vitro activity toward human 11 beta-HSD1, selectivity against 11 beta-HSD2, microsomal stability, and pharmacokinetic and safety profiles (hERG, CYP, and acute toxicity). Additionally, 18e exhibited good in vivo efficacy in rat and monkey models.

引用

页码：88 / 93

页数：6

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