Novel trans-2-aryl-cyclopropylamine analogues as potent and selective dipeptidyl peptidase IV inhibitors |
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Authors: | Ting-Yueh Tsai Tsu Hsu Chiung-Tong Chen Jai-Hong Cheng Teng-Kuang Yeh Xin Chen Chung-Yu Huang Chung-Nien Chang Kai-Chia Yeh Su-Huei Hsieh Chia-Hui Chien Yi-Wei Chang Chih-Hsiang Huang Yu-Wen Huang Chen-Lung Huang Ssu-Hui Wu Min-Hsien Wang Cheng-Tai Lu Yu-Sheng Chao Weir-Torn Jiaang |
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Institution: | Division of Biotechnology and Pharmaceutical Research, National Health Research Institutes, No. 35, Keyan Rd., Zhunan Town, Miaoli Country 350, Taiwan, ROC |
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Abstract: | A series of trans-2-aryl-cyclopropylamine derived compounds were synthesized and evaluated their biological activities against DPP-IV. The structure-activity relationships (SAR) led to the discovery of novel series of DPP-IV inhibitors, having IC50 values of <100 nM with excellent selectivity over the closely related enzymes, DPP8, DPP-II and FAP. The studies identified a potent and selective DPP-IV inhibitor 24b, which exhibited the ability to both significantly inhibit plasma DPP-IV activity in rats and improve glucose tolerance in lean mice and diet induced obese mice. |
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