Discovery and biological evaluation of adamantyl amide 11β-HSD1 inhibitors

A series of adamantyl amide 11β-HSD1 inhibitors has been discovered and chemically modified. Selected compounds are selective for 11β-HSD1 over 11β-HSD2 and possess excellent cellular potency in human and murine 11β-HSD1 assays. Good pharmacodynamic characteristics are observed in ex vivo assays.

The synthesis and biological activity of a series of adamantyl amide 11β-HSD1 inhibitors represented by 5 is reported.Figure optionsDownload as PowerPoint slide