(2 S, 3 S)-3-Amino-4-(3, 3-difluoropyrrolidin-1-yl)-N, N-dimethyl-4-oxo-2-(4-[1, 2, 4] triazolo [1, 5-a]-pyridin-6-ylphenyl) butanamide: A Selective α-Amino Amide …

…, M Beconi, J Di Salvo, GJ Eiermann, H He…

文献索引：Edmondson, Scott D.; Mastracchio, Anthony; Mathvink, Robert J.; He, Jiafang; Harper, Bart; Park, You-Jung; Beconi, Maria; Di Salvo, Jerry; Eiermann, George J.; He, Huaibing; Leiting, Barbara; Leone, Joseph F.; Levorse, Dorothy A.; Lyons, Kathryn; Patel, Reshma A.; Patel, Sangita B.; Petrov, Aleksandr; Scapin, Giovanna; Shang, Jackie; Roy, Ranabir Sinha; Smith, Aaron; Wu, Joseph K.; Xu, Shiyao; Zhu, Bing; Thornberry, Nancy A.; Weber, Ann E. Journal of Medicinal Chemistry, 2006 , vol. 49, # 12 p. 3614 - 3627

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被引用次数: 91

摘要

A series of β-substituted biarylphenylalanine amides were synthesized and evaluated as inhibitors of dipeptidyl peptidase IV (DPP-4) for the treatment of type 2 diabetes. Optimization of the metabolic profile of early analogues led to the discovery of (2 S, 3 S)-3- amino-4-(3, 3-difluoropyrrolidin-1-yl)-N, N-dimethyl-4-oxo-2-(4-[1, 2, 4] triazolo [1, 5-a] pyridin-6-ylphenyl) butanamide (6), a potent, orally active DPP-4 inhibitor (IC50= 6.3 nM) ...