【文章名】Discovery of Novel, Potent Benzamide Inhibitors of 11b-Hydroxysteroid Dehydrogenase Type 1 (11b-HSD1) Exhibiting Oral Activity in an Enzyme Inhibition ex Vivo Model.
Discovery of Novel, Potent Benzamide Inhibitors of 11b-Hydroxysteroid Dehydrogenase Type 1 (11b-HSD1) Exhibiting Oral Activity in an Enzyme Inhibition ex Vivo Model.
[摘要]：The authors report the discovery of potent benzamide inhibitors of 11b-hydroxysteroid dehydrogenase (11b-HSD1). The optimization and correlation of in vitro and in vivo metabolic stability will be described. Through modifications to the initial lead 2, the authors discovered pyridyl compd. (I). This compd. has a favorable pharmacokinetic profile across three species and showed a dose-dependent decrease in adipose 11b-HSD1 activity in a monkey ex vivo pharmacodynamic model.
