| Title : Discovery of 3-aminopiperidines as potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitors - Cox_2007_Bioorg.Med.Chem.Lett_17_4579 |
| Author(s) : Cox JM , Harper B , Mastracchio A , Leiting B , Sinha Roy R , Patel RA , Wu JK , Lyons KA , He H , Xu S , Zhu B , Thornberry NA , Weber AE , Edmondson SD |
| Ref : Bioorganic & Medicinal Chemistry Lett , 17 :4579 , 2007 |
|
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. |
| PubMedSearch : Cox_2007_Bioorg.Med.Chem.Lett_17_4579 |
| PubMedID: 17562364 |
Cox JM, Harper B, Mastracchio A, Leiting B, Sinha Roy R, Patel RA, Wu JK, Lyons KA, He H, Xu S, Zhu B, Thornberry NA, Weber AE, Edmondson SD (2007)
Discovery of 3-aminopiperidines as potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitors
Bioorganic & Medicinal Chemistry Lett
17 :4579
Cox JM, Harper B, Mastracchio A, Leiting B, Sinha Roy R, Patel RA, Wu JK, Lyons KA, He H, Xu S, Zhu B, Thornberry NA, Weber AE, Edmondson SD (2007)
Bioorganic & Medicinal Chemistry Lett
17 :4579