Author/Authors :
Jin-Hee Ahn، نويسنده , , Mi Sik Shin، نويسنده , , Mi Ae Jun، نويسنده , , Sun Ho Jung، نويسنده , , Seung Kyu Kang، نويسنده , , Kwang Rok Kim، نويسنده , , Sang Dal Rhee، نويسنده , , Nam Sook Kang، نويسنده , , Sun Young Kim، نويسنده , , Sang-Kwon Sohn، نويسنده , , Sung Gyu Kim، نويسنده , , Mi Sun Jin، نويسنده , , Jie-Oh Lee، نويسنده , , Hyae Gyeong Cheon، نويسنده , , Sung-Soo Kim، نويسنده ,
Abstract :
Inhibitors of dipeptidyl peptidase IV (DPP-IV) have been shown to be effective treatments for type 2 diabetes. A series of β-aminoacyl-containing cyclic hydrazine derivatives were synthesized and evaluated as DPP-IV inhibitors. One member of this series, (R)-3-amino-1-(2-benzoyl-1,2-diazepan-1-yl)-4-(2,4,5-trifluorophenyl)butan-1-one (10f), showed potent in vitro activity, good selectivity and in vivo efficacy in mouse models. Also, the binding mode of compound 10f was determined by X-ray crystallography.
