Synthesis and structural activity relationship of 11β-HSD1 inhibitors with novel adamantane replacements

A series of structurally novel and metabolically stable bridged bicyclic carbocycle and heterocycle adamantane replacements have been synthesized and biologically evaluated. Several of these compounds exhibit excellent human and mouse 11β-HSD1 potency and 11β-HSD2 selectivity.

A series of structurally novel and metabolically stable bridged bicyclic carbocycle and heterocycle adamantane replacements have been synthesized and biologically evaluated. Several of these compounds exhibit excellent human and mouse 11β-HSD1 potency and 11β-HSD2 selectivity.Figure optionsDownload as PowerPoint slide