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 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.

Graphical abstractVarious 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.Figure optionsDownload full-size imageDownload as PowerPoint slide