Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1375282 | Bioorganic & Medicinal Chemistry Letters | 2009 | 5 Pages |
Abstract
A series of (2S)-cyanopyrrolidines with glutamic acid derivatives at the P2 site have been prepared and evaluated as inhibitors of dipeptidyl peptidase IV (DPP-IV). The structure–activity relationships (SAR) led to the discovery of potent 3-substituted glutamic acid analogues, providing enhanced chemical stability and excellent selectivity over the closely related enzymes, DPP8, DPP-II and FAP. Compound 13f exhibited the ability to both significantly decrease the glucose excursion and inhibit plasma DPP-IV activity.
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Ting-Yueh Tsai, Tsu Hsu, Chiung-Tong Chen, Jai-Hong Cheng, Mei-Chun Chiou, Chih-Hsiang Huang, Ya-Ju Tseng, Teng-Kuang Yeh, Chung-Yu Huang, Kai-Chia Yeh, Yu-Wen Huang, Ssu-Hui Wu, Min-Hsien Wang, Xin Chen, Yu-Sheng Chao, Weir-Torn Jiaang,