Synthesis, biological evaluation and structural determination of β-aminoacyl-containing cyclic hydrazine derivatives as dipeptidyl peptidase IV (DPP-IV) inhibitors
| Autor: | Sun Ho Jung, Mi Ae Jun, Jie Oh Lee, Nam Sook Kang, Sung Gyu Kim, Sang-Kwon Sohn, Sun Young Kim, Seung Kyu Kang, Mi Sik Shin, Hyae Gyeong Cheon, Mi Sun Jin, Jin Hee Ahn, Sang Dal Rhee, Sung-Soo Kim, Kwang Rok Kim |
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| Rok vydání: | 2007 |
| Předmět: |
Stereochemistry
Chemistry Pharmaceutical Clinical Biochemistry Molecular Conformation Pharmaceutical Science Crystallography X-Ray Biochemistry Dipeptidyl peptidase Inhibitory Concentration 50 Mice Glucagon-Like Peptide 1 In vivo Drug Discovery Animals Enzyme Inhibitors Molecular Biology Hydrazine derivatives Biological evaluation Dipeptidyl-Peptidase IV Inhibitors Dpp iv inhibitors Chemistry Organic Chemistry In vitro Protein Structure Tertiary Mice Inbred C57BL Kinetics Hydrazines Models Chemical Drug Design Molecular Medicine Selectivity |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 17:2622-2628 |
| ISSN: | 0960-894X |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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