Design, synthesis, and biological evaluation of triazolopiperazine-based β-amino amides as potent, orally active dipeptidyl peptidase IV (DPP-4) inhibitors

Various β-amino amides containing triazolopiperazine heterocycles have been prepared and evaluated as dipeptidyl peptidase IV (DPP-4) inhibitors. The in vitro profile of these compounds is described, and in vivo efficacy and pharmacokinetics are also presented. 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.