Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1393399 | European Journal of Medicinal Chemistry | 2008 | 14 Pages |
Abstract
A series of pyrazoline derivatives with β-amino acyl group were synthesized and evaluated for their ability to inhibit dipeptidyl peptidase IV. Several pyrazoline derivatives exhibited submicromolar inhibitory activities against DPP-IV. X-ray co-crystal structure of initial hit compound 1h was determined. Among this series, carboxylic acid substituted pyrazoline derivative 2u was the most active and greatly decreased the inhibitory activity toward CYP3A4 enzyme.
Graphical abstractFigure optionsDownload full-size imageDownload as PowerPoint slide
Keywords
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Mi Ae Jun, Woul Seong Park, Seung Kyu Kang, Ki Young Kim, Kwang Rok Kim, Sang Dal Rhee, Myung Ae Bae, Nam Sook Kang, Sang-Kwon Sohn, Sung Gyu Kim, Jie Oh Lee, Duck Hyung Lee, Hyae Gyeong Cheon, Sung Soo Kim, Jin Hee Ahn,