β-Keto sulfones as inhibitors of 11β-hydroxysteroid dehydrogenase type I and the mechanism of action

Jason Xiang,Manus Ipek,Vipin Suri,May Tam,Yuzhe Xing,Nelson Huang,Yanling Zhang,James Tobin,Tarek S. Mansour,John McKew

Bioorganic & Medicinal Chemistry（2007）

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摘要

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.

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关键词

HSD1,11β-HSD1,Diabetes,Metabolic syndrome,Keto sulfone,Synthesis

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