195617-73-3Relevant articles and documents
Novel trans-2-aryl-cyclopropylamine analogues as potent and selective dipeptidyl peptidase IV inhibitors
Tsai, Ting-Yueh,Hsu, Tsu,Chen, Chiung-Tong,Cheng, Jai-Hong,Yeh, Teng-Kuang,Chen, Xin,Huang, Chung-Yu,Chang, Chung-Nien,Yeh, Kai-Chia,Hsieh, Su-Huei,Chien, Chia-Hui,Chang, Yi-Wei,Huang, Chih-Hsiang,Huang, Yu-Wen,Huang, Chen-Lung,Wu, Ssu-Hui,Wang, Min-Hsien,Lu, Cheng-Tai,Chao, Yu-Sheng,Jiaang, Weir-Torn
experimental part, p. 2388 - 2399 (2009/09/05)
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.
