| Title : Design, synthesis, and biological evaluation of triazolopiperazine-based beta-amino amides as potent, orally active dipeptidyl peptidase IV (DPP-4) inhibitors - Kowalchick_2007_Bioorg.Med.Chem.Lett_17_5934 |
| 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 |
| Ref : Bioorganic & Medicinal Chemistry Lett , 17 :5934 , 2007 |
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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. |
| PubMedSearch : Kowalchick_2007_Bioorg.Med.Chem.Lett_17_5934 |
| PubMedID: 17827003 |
| Gene_locus related to this paper: human-DPP4 |
| Inhibitor | Triazolopiperazine-based-beta-amino-acid |
| Gene_locus | human-DPP4 |
| Structure | 2QOE |
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 (2007)
Design, synthesis, and biological evaluation of triazolopiperazine-based beta-amino amides as potent, orally active dipeptidyl peptidase IV (DPP-4) inhibitors
Bioorganic & Medicinal Chemistry Lett
17 :5934
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 (2007)
Bioorganic & Medicinal Chemistry Lett
17 :5934