Structure Report for: 2QOE

Kowalchick, J.E., Leiting, B., Pryor, K.D., Marsilio, F., Wu, J.K., He, H., Lyons, K.A., Eiermann, G.J., Petrov, A., Scapin, G. et al.

Title: Design, synthesis, and biological evaluation of triazolopiperazine-based beta-amino amides as potent, orally active dipeptidyl peptidase IV (DPP-4) inhibitors
Kowalchick JE, Leiting B, Pryor KD, Marsilio F, Wu JK, He H, Lyons KA, Eiermann GJ, Petrov A and Kim D <4 more author(s)> Kowalchick JE, Leiting B, Pryor KD, Marsilio F, Wu JK, He H, Lyons KA, Eiermann GJ, Petrov A, Scapin G, Patel RA, Thornberry NA, Weber AE, Kim D (- 4)
Ref: Bioorganic & Medicinal Chemistry Lett, 17:5934, 2007 : PubMed
Abstract


ESTHER: Kowalchick_2007_Bioorg.Med.Chem.Lett_17_5934
PubMedSearch: Kowalchick 2007 Bioorg.Med.Chem.Lett 17 5934
PubMedID: 17827003
Gene_locus related to this paper: human-DPP4
Inhibitor(s) related to this paper: Triazolopiperazine-based-beta-amino-acid

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.