Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1375594 | Bioorganic & Medicinal Chemistry Letters | 2009 | 6 Pages |
Abstract
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.
Graphical abstractThe 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.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
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Authors
Daqing Sun, Zhulun Wang, Mario Cardozo, Rebekah Choi, Michael DeGraffenreid, Yongmei Di, Xiao He, Juan C. Jaen, Marc Labelle, Jinsong Liu, Ji Ma, Shichang Miao, Athena Sudom, Liang Tang, Hua Tu, Stefania Ursu, Nigel Walker, Xuelei Yan, Qiuping Ye,