Piperidine amides as 11β-hydroxysteroid dehydrogenase type 1 inhibitors

A series of piperidine amide inhibitors of human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) were identified via modifications of the HTS hit compound 1. The synthesis, in vitro biological evaluation, and structure–activity relationship of these compounds are presented.

Compound 1 was identified as a potent 11β-HSD1 inhibitor in a HTS screen. Synthesis and inhibitory potency of analogs to 1 are reported.Figure optionsDownload as PowerPoint slide