The synthesis and SAR of novel diarylsulfone 11β-HSD1 inhibitors
In this communication, human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitory activities of a novel series of diarylsulfones are described. Optimization of this series resulted in several highly potent 11β-HSD1 inhibitors with excellent pharmacokinetic (PK) properties. Compound (S)-25 showed excellent efficacy in a non-human primate ex vivo pharmacodynamic model.
Yan, Xuelei,Wang, Zhulun,Sudom, Athena,Cardozo, Mario,Degraffenreid, Michael,Di, Yongmei,Fan, Pingchen,He, Xiao,Jaen, Juan C.,Labelle, Marc,Liu, Jinsong,Ma, Ji,McMinn, Dustin,Miao, Shichang,Sun, Daqing,Tang, Liang,Tu, Hua,Ursu, Stefania,Walker, Nigel,Ye, Qiuping,Powers, Jay P.
scheme or table
p. 7071 - 7075
(2011/01/03)
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