Title of article :
Design, synthesis, and biological evaluation of triazolopiperazine-based β-amino amides as potent, orally active dipeptidyl peptidase IV (DPP-4) inhibitors
Author/Authors :
Jennifer E. Kowalchick، نويسنده , , Barbara Leiting، نويسنده , , KellyAnn D. Pryor، نويسنده , , Frank Marsilio، نويسنده , , Joseph K. Wu، نويسنده , , Huaibing He، نويسنده , , Kathryn A. Lyons، نويسنده , , George J. Eiermann، نويسنده , , Aleksandr Petrov، نويسنده , , Giovanna Scapin، نويسنده , , Reshma A. Patel، نويسنده , , Nancy A. Thornberry، نويسنده , , Ann E. Weber، نويسنده , , Dooseop Kim، نويسنده ,
Abstract :
Various β-amino amides containing triazolopiperazine heterocycles have been prepared and evaluated as potent, selective, orally active dipeptidyl peptidase IV (DPP-4) inhibitors. These compounds display excellent oral bioavailability and good overall pharmacokinetic profiles in preclinical species. Moreover, in vivo efficacy in an oral glucose tolerance test in lean mice is demonstrated.
Keywords :
Dipeptidyl peptidase IV , DPP-4 , Dipeptidyl peptidase IV inhibitors , ?-Amino amides , Triazolopiperazine , DPP-4 inhibitors , type 2 diabetes , Triazolopiperazine-based ?-amino amides
