Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10588813 | Bioorganic & Medicinal Chemistry Letters | 2010 | 5 Pages |
Abstract
A series of 2-[3-[2-[(2S)-2-cyano-1-pyrrolidinyl]-2-oxoethylamino]-3-methyl-1-oxobutyl]-based DPP-IV inhibitors with various monocyclic amines were synthesized. The structure-activity relationships (SAR) led to the discovery of potent DPP-IV inhibitors, having IC50 values of <100 nM with excellent selectivity over the closely related enzymes, DPP-II, DPP8, DPP9 and FAP (IC50 > 20 μM). Of these compounds, the analogues 12a, 12h and 12i exhibited a long-lasting ex vivo DPP-IV inhibition in rats.
Keywords
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Teng-Kuang Yeh, Ting-Yueh Tsai, Tsu Hsu, Jai-Hong Cheng, Xin Chen, Jen-Shin Song, Horng-Shing Shy, Mei-Chun Chiou, Chia-Hui Chien, Ya-Ju Tseng, Chung-Yu Huang, Kai-Chia Yeh, Yu-Lin Huang, Chih-Hsiang Huang, Yu-Wen Huang, Min-Hsien Wang, Hung-Kuan Tang,