Title of article :
Discovery of 3-aminopiperidines as potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitors
Author/Authors :
Jason M. Cox، نويسنده , , Bart Harper، نويسنده , , Anthony Mastracchio، نويسنده , , Barbara Leiting، نويسنده , , Ranabir Sinha-Roy، نويسنده , , Reshma A. Patel، نويسنده , , Joseph K. Wu، نويسنده , , Kathryn A. Lyons، نويسنده , , Huaibing He، نويسنده , , Shiyao Xu، نويسنده , , Bing Zhu، نويسنده , , Nancy A. Thornberry، نويسنده , , Ann E. Weber، نويسنده , , Scott D. Edmondson، نويسنده ,
Abstract :
Substituted 3-aminopiperidines 3 were evaluated as DPP-4 inhibitors. The inhibitors showed good DPP-4 potency with superb selectivity over other peptidases (QPP, DPP8, and DPP9). Selected DPP-4 inhibitors were further evaluated for their hERG potassium channel, calcium channel, Cyp2D6, and pharmacokinetic profiles.
Keywords :
DPP-4 , DPP9 , QPP , DPP8 , Aminopiperidine , Dipeptidyl peptidase IV
