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 ...
[Gooden, David M.; Schmidt, Dawn M.Z.; Pollock, Julie A.; Kabadi, Ami M.; McCafferty, Dewey G. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 10 p. 3047 - 3051]
