917769-72-3Relevant academic research and scientific papers
Discovery of novel, potent benzamide inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) exhibiting oral activity in an enzyme inhibition ex vivo model
Julian, Lisa D.,Wang, Zhulun,Bostick, Tracy,Caille, Seb,Choi, Rebekah,DeGraffenreid, Michael,Di, Yongmei,He, Xiao,Hungate, Randall W.,Jaen, Juan C.,Liu, Jinsong,Monshouwer, Mario,McMinn, Dustin,Rew, Yosup,Sudom, Athena,Sun, Daqing,Tu, Hua,Ursu, Stefania,Walker, Nigel,Yan, Xuelei,Ye, Qiuping,Powers, Jay P.
, p. 3953 - 3960 (2008)
We report the discovery of potent benzamide inhibitors of 11β-hydroxysteroid dehydrogenase (11β-HSD1). The optimization and correlation of in vitro and in vivo metabolic stability will be described. Through modifications to our initial lead 2, we discovered pyridyl compound 13. This compound has a favorable pharmacokinetic profile across three species and showed a dose-dependent decrease in adipose 11β-HSD1 activity in a monkey ex vivo pharmacodynamic model.
