Adamantane sulfone and sulfonamide 11-β-HSD1 Inhibitors

Potent and selective adamantane sulfone and sulfonamide inhibitors of 11-β-HSD-1 have been discovered. Selected compounds from these series have robust pharmacokinetic profiles and strongly inhibit liver, fat, and brain HSD1 for extended periods after oral dosing.

The synthesis of potent and selective adamantane sulfone and sulfonamide 11-β-HSD-1 inhibitors represented by 10 and 40 is reported.Figure optionsDownload as PowerPoint slide