The synthesis and SAR of novel diarylsulfone 11β-HSD1 inhibitors.

Bioorganic & Medicinal Chemistry Letters（2010）

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摘要

The synthesis and SAR of a series of diarylsulfone inhibitors of 11β-HSD1 are described. Optimization rapidly led to potent, selective, and orally bioavailable inhibitors demonstrating efficacy in a non-human primate ex vivo enzyme inhibition model.

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关键词

11β-HSD1,11β-HSD2,Diabetes,Metabolic syndrome,Hydroxysteroid dehydrogenase,Diarylsulfones

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