作为二肽基肽酶IV抑制剂的三唑并哌嗪酰胺：佳维乐（磷酸西他列汀）的紧密类似物。
Triazolopiperazine-amides as dipeptidyl peptidase IV inhibitors: close analogs of JANUVIA (sitagliptin phosphate).
作者信息
Kim Dooseop, Kowalchick Jennifer E, Edmondson Scott D, Mastracchio Anthony, Xu Jinyou, Eiermann George J, Leiting Barbara, Wu Joseph K, Pryor KellyAnn D, Patel Reshma A, He Huaibing, Lyons Kathryn A, Thornberry Nancy A, Weber Ann E
机构信息
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 2000, Rahway, NJ 07065, USA.
出版信息
Bioorg Med Chem Lett. 2007 Jun 15;17(12):3373-7. doi: 10.1016/j.bmcl.2007.03.098. Epub 2007 Apr 5.
A series of beta-aminoamides bearing triazolopiperazines has been prepared and evaluated as potent, selective, orally active dipeptidyl peptidase IV (DPP-4) inhibitors. Efforts at optimization of the beta-aminoamide series, which ultimately led to the discovery of JANUVIA (sitagliptin phosphate, compound 1), are described.
一系列带有三唑并哌嗪的β-氨基酰胺已被制备并作为强效、选择性、口服活性二肽基肽酶IV（DPP-4）抑制剂进行评估。本文描述了对β-氨基酰胺系列进行优化的工作，这些工作最终促成了JANUVIA（磷酸西他列汀，化合物1）的发现。
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