| Title : Synthesis, biological evaluation and structural determination of beta-aminoacyl-containing cyclic hydrazine derivatives as dipeptidyl peptidase IV (DPP-IV) inhibitors - Ahn_2007_Bioorg.Med.Chem.Lett_17_2622 |
| Author(s) : Ahn JH , Shin MS , Jun MA , Jung SH , Kang SK , Kim KR , Rhee SD , Kang NS , Kim SY , Sohn SK , Kim SG , Jin MS , Lee JO , Cheon HG , Kim SS |
| Ref : Bioorganic & Medicinal Chemistry Lett , 17 :2622 , 2007 |
|
Abstract :
Inhibitors of dipeptidyl peptidase IV (DPP-IV) have been shown to be effective treatments for type 2 diabetes. A series of beta-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. |
| PubMedSearch : Ahn_2007_Bioorg.Med.Chem.Lett_17_2622 |
| PubMedID: 17331715 |
| Gene_locus related to this paper: human-DPP4 |
| Inhibitor | Cyclic-Hydrazine-Derivative |
| Gene_locus | human-DPP4 |
| Structure | 2OLE |
Ahn JH, Shin MS, Jun MA, Jung SH, Kang SK, Kim KR, Rhee SD, Kang NS, Kim SY, Sohn SK, Kim SG, Jin MS, Lee JO, Cheon HG, Kim SS (2007)
Synthesis, biological evaluation and structural determination of beta-aminoacyl-containing cyclic hydrazine derivatives as dipeptidyl peptidase IV (DPP-IV) inhibitors
Bioorganic & Medicinal Chemistry Lett
17 :2622
Ahn JH, Shin MS, Jun MA, Jung SH, Kang SK, Kim KR, Rhee SD, Kang NS, Kim SY, Sohn SK, Kim SG, Jin MS, Lee JO, Cheon HG, Kim SS (2007)
Bioorganic & Medicinal Chemistry Lett
17 :2622