939964-16-6Relevant articles and documents
Synthesis, biological evaluation and structural determination of β-aminoacyl-containing cyclic hydrazine derivatives as dipeptidyl peptidase IV (DPP-IV) inhibitors
Ahn, Jin Hee,Shin, Mi Sik,Jun, Mi Ae,Jung, Sun Ho,Kang, Seung Kyu,Kim, Kwang Rok,Rhee, Sang Dal,Kang, Nam Sook,Kim, Sun Young,Sohn, Sang-Kwon,Kim, Sung Gyu,Jin, Mi Sun,Lee, Jie Oh,Cheon, Hyae Gyeong,Kim, Sung Soo
, p. 2622 - 2628 (2007)
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)but an-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.