Title of article :
4,5-Dihydro-4-oxo-3H-imidazo[4,5-c]pyridines: potent arylacetic acid-derived AT1 antagonists with improved affinity for the AT2 receptor
Author/Authors :
Werner W. K. R. Mederski، نويسنده , , Dieter Dorsch، نويسنده , , Mathias Osswald، نويسنده , , Norbert Beier، نويسنده , , Ingeborg Lues، نويسنده , , Klaus-Otto Minck، نويسنده , , Pierre Schelling، نويسنده , , Bernhard J. Ladstetter، نويسنده ,
Abstract :
The replacement of dimethylacetamide with arylacetic acid esters and acetamides at the imidazo[4,5-c]pyridine 5-position of EMD 66684 2 imparts affinity for the AT2 receptor. The highest affinity was found with the phenylacetic acid isopropylester moiety, which led to compound 7c with an IC50 value of 32 nM (AT2) and an AT2/AT1 ratio of 5.
