Author/Authors :
Jens-Uwe Peters، نويسنده , , Silja Weber، نويسنده , , Stéphane Kritter، نويسنده , , Peter Weiss، نويسنده , , Angelina Wallier، نويسنده , , Markus Boehringer، نويسنده , , Michael Hennig، نويسنده , , Bernd Kuhn، نويسنده , , Bernd-Michael Loeffler، نويسنده ,
Abstract :
The influence of aromatic substitution on a newly discovered class of inhibitors of dipeptidyl peptidase IV was investigated. A 105-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.