Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1369558 | Bioorganic & Medicinal Chemistry Letters | 2014 | 5 Pages |
A series of novel aminomethyl-piperidones were designed and evaluated as potential DPP-IV inhibitors. Optimized analogue 12v ((4S,5S)-5-(aminomethyl)-1-(2-(benzo[d][1,3]dioxol-5-yl)ethyl)-4-(2,5-difluorophenyl)piperidin-2-one) showed excellent in vitro potency and selectivity for DPP-IV over other serine proteases. The lead compound 12v showed potent and long acting antihyperglycemic effects (in vivo), along with improved pharmacokinetic profile.
Graphical abstractA series of novel aminomethyl-piperidones were designed and evaluated as potential DPP-IV inhibitors. The lead compound 12v ((4S,5S)-5-(aminomethyl)-1-(2-(benzo[d][1,3]dioxol-5-yl)ethyl)-4-(2,5-difluorophenyl)piperidin-2-one) showed potent and long acting antihyperglycemic effects (in vivo), along with improved pharmacokinetic profile.Figure optionsDownload full-size imageDownload as PowerPoint slide