Design, synthesis, and biological evaluation of triazolopiperazine-based beta-amino amides as potent, orally active dipeptidyl peptidase IV (DPP-4) inhibitors |
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| Authors: | Kowalchick Jennifer E Leiting Barbara Pryor KellyAnn D Marsilio Frank Wu Joseph K He Huaibing Lyons Kathryn A Eiermann George J Petrov Aleksandr Scapin Giovanna Patel Reshma A Thornberry Nancy A Weber Ann E Kim Dooseop |
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| Institution: | Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA. jennifer_kowalchick@yahoo.com |
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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. |
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