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The design of potent and selective inhibitors of DPP-4: Optimization of ADME properties by amide replacements |
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| Authors: | Sonja Nordhoff Stephan Bulat Silvia Cerezo-Glvez Oliver Hill Barbara Hoffmann-Enger Meritxell Lpez-Canet Claudia Rosenbaum Christian Rummey Meinolf Thiemann Victor G Matassa Paul J Edwards Achim Feurer |
| Institution: | aSanthera Pharmaceuticals (Switzerland) Ltd, Hammerstrasse 47, CH-4410 Liestal, Switzerland |
| 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. |
| Keywords: | Dipeptidyl peptidase IV DPP-IV DPP-4 Type 2 diabetes Glucagon-like peptide 1 GLP-1 |
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