- The design of potent and selective inhibitors of DPP-4: optimization of ADME properties by amide replacements.
The design of potent and selective inhibitors of DPP-4: optimization of ADME properties by amide replacements.
Bioorganic & medicinal chemistry letters (2009-10-17)
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
PMID19833514
摘要
For a series of beta-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.