Discovery of orally active butyrolactam 11β-HSD1 inhibitors

A series of metabolically stable butyrolactam 11β-HSD1 inhibitors have been synthesized and biologically evaluated. These compounds exhibit excellent HSD1 potency and HSD2 selectivity, pharmacokinetic, and pharmacodynamic profiles.

A series of metabolically stable butyrolactam 11β-HSD1 inhibitors have been synthesized and biologically evaluated.Figure optionsDownload as PowerPoint slide