The design of potent and selective inhibitors of DPP-4: Optimization of ADME properties by amide replacements

Sonja Nordhoff, Stephan Bulat, Silvia Cerezo-Gálvez, Oliver Hill, Barbara Hoffmann-Enger, Meritxell López-Canet, Claudia Rosenbaum, Christian Rummey, Meinolf Thiemann, Victor G. Matassa, Paul J. Edwards, Achim Feurer, Sonja Nordhoff, Stephan Bulat, Silvia Cerezo-Gálvez, Oliver Hill, Barbara Hoffmann-Enger, Meritxell López-Canet, Claudia Rosenbaum, Christian Rummey, Meinolf Thiemann, Victor G. Matassa, Paul J. Edwards, Achim Feurer

Index: Bioorg. Med. Chem. Lett. 19(22) , 6340-5, (2009)

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Abstract

For a series of β-homophenylalanine based inhibitors of dipeptidyl peptidase IV ADME properties were improved by the incorporation of amide replacements. These efforts led to a novel series of potent and selective inhibitors of DPP-4 that exhibit an attractive pharmacokinetic profile and show excellent efficacy in an animal model of diabetes.