Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1399672 | European Journal of Medicinal Chemistry | 2009 | 5 Pages |
Abstract
To find potent and selective inhibitors of dipeptidyl peptidase IV (DPP-IV), we synthesized a series of 2-cyanopyrrolidine derivatives with constrained imidazolidin ring and tested their activities against DPP-IV. Most of them exhibited submicromolar inhibitory activities against DPP-IV. The most potent compound among these is (S)-1-(2-(2-(3-(3,4-dimethoxyphenyl)-2-oxoimidazolidin-1-yl)ethyl-amino)acetyl)pyrrolidine-2-carbonitrile (6n), which is a 2 nM DPP-IV inhibitor.
Graphical abstractR = 3,4-Dimethoxyphenyl, DPP-IV IC50 = 2.0 nMFigure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Liutang Wang, Bin Zhang, Jianxin Ji, Bogang Li, Jufang Yan, Weiyu Zhang, Yong Wu, Xuechao Wang,