Synthesis and biological evaluation of heterocycle containing adamantane 11β-HSD1 inhibitors

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

A series of metabolically stable adamantane amide 11β-HSD1 inhibitors have been synthesized and biologically evaluated. These compounds exhibit excellent HSD1 potency and HSD2 selectivity and good pharmacokinetic and pharmacodynamic profiles.Figure optionsDownload as PowerPoint slide