Abstract
Various beta-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.
MeSH terms
-
Amides / chemical synthesis
-
Amides / chemistry*
-
Amides / pharmacokinetics
-
Amides / pharmacology*
-
Animals
-
Crystallography, X-Ray
-
Dipeptidyl-Peptidase IV Inhibitors*
-
Drug Design
-
Drug Evaluation, Preclinical
-
Models, Molecular
-
Piperazines / chemistry*
-
Protease Inhibitors / chemical synthesis
-
Protease Inhibitors / chemistry*
-
Protease Inhibitors / pharmacokinetics
-
Protease Inhibitors / pharmacology*
-
Rats
Substances
-
Amides
-
Dipeptidyl-Peptidase IV Inhibitors
-
Piperazines
-
Protease Inhibitors