Oxazolones as potent inhibitors of 11β-hydroxysteroid dehydrogenase type 1

2,5,5-Trisubstituted oxazolones were identified as potent inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1). The synthesis, structure–activity relationship and metabolic stability of these compounds are presented.

Compounds of general formula 1 were found to be potent inhibitors of 11β-HSD1. Synthesis, structure–activity relationship and metabolic stability of these compounds are reported.Figure optionsDownload as PowerPoint slide