- From lead to preclinical candidate: optimization of beta-homophenylalanine based inhibitors of dipeptidyl peptidase IV.
From lead to preclinical candidate: optimization of beta-homophenylalanine based inhibitors of dipeptidyl peptidase IV.
Bioorganic & medicinal chemistry letters (2009-07-07)
Sonja Nordhoff, Meritxell López-Canet, Barbara Hoffmann-Enger, Stephan Bulat, Silvia Cerezo-Gálvez, Oliver Hill, Claudia Rosenbaum, Christian Rummey, Meinolf Thiemann, Victor G Matassa, Paul J Edwards, Achim Feurer
PMID19576767
摘要
A series of highly potent and selective inhibitors of DPP-4 was optimized for ADMET properties. The effort resulted in the discovery of inhibitor 1g, that exhibits excellent efficacy in an oral glucose tolerance test and an attractive pharmacokinetic profile.