1144517-76-9Relevant academic research and scientific papers
Synthesis and optimization of arylsulfonylpiperazines as a novel class of inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1)
Sun, Daqing,Wang, Zhulun,Cardozo, Mario,Choi, Rebekah,DeGraffenreid, Michael,Di, Yongmei,He, Xiao,Jaen, Juan C.,Labelle, Marc,Liu, Jinsong,Ma, Ji,Miao, Shichang,Sudom, Athena,Tang, Liang,Tu, Hua,Ursu, Stefania,Walker, Nigel,Yan, Xuelei,Ye, Qiuping,Powers, Jay P.
scheme or table, p. 1522 - 1527 (2009/12/07)
The synthesis and SAR of a series of arylsulfonylpiperazine inhibitors of 11β-HSD1 are described. Optimization rapidly led to potent, selective, and orally bioavailable inhibitors demonstrating efficacy in a cynomolgus monkey ex vivo enzyme inhibition model.
