Aminomethylpyrimidines as novel DPP-IV inhibitors: a 10(5)-fold activity increase by optimization of aromatic substituents |
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| Authors: | Peters Jens-Uwe Weber Silja Kritter Stéphane Weiss Peter Wallier Angelina Boehringer Markus Hennig Michael Kuhn Bernd Loeffler Bernd-Michael |
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| Institution: | Pharma Division, Preclinical Research, F. Hoffmann-La Roche Ltd, CH-4070 Basel, Switzerland. jens-uwe.peters@roche.com |
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| Abstract: | The influence of aromatic substitution on a newly discovered class of inhibitors of dipeptidyl peptidase IV was investigated. A 10(5)-fold increase in potency was achieved by the optimization of aromatic substituents in a parallel chemistry program. The observed SAR could be explained by an X-ray structure of the protein-ligand complex. |
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