β-Keto sulfones as inhibitors of 11β-hydroxysteroid dehydrogenase type I and the mechanism of action
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- 作者：Jason Xiang ; Manus Ipek ; Vipin Suri ; May Tam ; Yuzhe Xing ; Nelson Huang ; Yanling Zhang ; James Tobin ; Tarek S. Mansour ; John McKew
- 关键词：HSD1 ; 11β ; -HSD1 ; Diabetes ; Metabolic syndrome ; Keto sulfone ; Synthesis
- 刊名：Bioorganic and Medicinal Chemistry
- 出版年：2007
- 出版时间：1 July 2007
- 年：2007
- 卷：15
- 期：13
- 页码：4396-4405
- 全文大小：224 K
文摘
The design, synthesis, and biological evaluation of β-keto sulfones as 11β-HSD1 inhibitors and the mechanism of inhibition are described here. This class of compounds is not active against 11β-HSD2 and therefore may have therapeutic potential for metabolic syndrome and type 2 diabetes.