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
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA.
Bioorg Med Chem Lett. 2007 Nov 1;17(21):5934-9. doi: 10.1016/j.bmcl.2007.07.100. Epub 2007 Aug 23.
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.
已制备了多种含三唑并哌嗪杂环的β-氨基酰胺，并将其作为强效、选择性、口服活性二肽基肽酶IV（DPP-4）抑制剂进行了评估。这些化合物在临床前物种中表现出优异的口服生物利用度和良好的整体药代动力学特征。此外，还证明了其在瘦小鼠口服葡萄糖耐量试验中的体内疗效。
