1472657-33-2Relevant academic research and scientific papers
Design and Synthesis of (R)-1-Arylsulfonylpiperidine-2-carboxamides as 11β-Hydroxysteroid Dehydrogenase Type1 Inhibitors
Xia, Guangxin,Liu, Lin,Liu, Haiyan,Yu, Jianxin,Xu, Zhenmin,Chen, Qian,Ma, Chen,Li, Ping,Xiong, Bing,Liu, Xuejun,Shen, Jingkang
supporting information, p. 577 - 581 (2013/08/22)
R adamantly beats S: 11β-HSD1 is a target for treating metabolic syndrome. The Risomer 5 was selected as a starting point for optimization and SAR studies. Inhibitor 8w emerged after several rounds of optimization, showing cross-species inhibition of human and mouse 11β-HSD1. It also displays a good DMPK profile invitro, and was advanced to PK/PD evaluations invivo. The results confirmed its dose-dependent activity in mice.
