ChemInform Abstract: A New Series of Imidazolones: Highly Specific and Potent Nonpeptide AT1 Angiotensin II Receptor Antagonists.

Abstract

A New Series of Imidazolones: Highly Specific and Potent Nonpeptide AT1 Angiotensin II Receptor Antagonists.-A series of novel dihydroimidazol-4-ones, e.g. (V)-(VII), is synthesized and tested in vivo for angiotensin II antagonism at the AT1 subtype receptor. The most active compounds found, i.e. (VI) and ( VII), show IC50 values in the lower nanomolar range. -(BERNHART, C. A.; PERREAUT, P. M.; FERRARI, B. P.; MUNEAUX, Y. A.; ASSENS, J.-L. A.; CLEMENT, J.; HAUDRICOURT, F.; MUNEAUX, C. F.; TAILLADES, J. E.; VIGNAL, M.-A.; GOUGAT, J.; GUIRAUDOU, P. R.; LACOUR, C. A.; ROCCON, A.; CAZAUBON, C. F.; BRELIERE, J.-C.; LE FUR, G.; NISATO, D.; J. Med. Chem. 36 (1993) 22, 3371-3380; Sanofi Rech., 34184 Montpellier, Fr.; EN)