ChemInform Abstract: Synthesis and Structure‐Activity of 4(5)‐(2,2‐Diphenylethyl)imidazoles as New α2‐Adrenoreceptor Antagonists.

Abstract

Synthesisand Structure-Activity of 4(5)-(2,2-Diphenylethyl)imidazoles as New α2-Adrenoreceptor Antagonists.-Some title compounds such as (III), (VI), (VIII) and (XI) are prepared in order to test their use as antagonists. The product (III) is a potent and selective α2-adrenoreceptor antagonist with additional activity as a norepinephrine uptake inhibitor. (VI) and ( VIIIa) show equivalent activity to (III), whereas (VIIIb) possesses no activity. Substitution of the imidazole ring results in an important loss of activity. Any modifications in the link between the diphenyl moiety and the imidazole ring lead to a reduction of antagonist properties (some yields not given). -(CORDI, A. A.; SNYERS, M. P.; GIRAUD-MANGIN, D.; VAN DER MAESEN, C.; VAN HOECK, J. P.; BEUZE, S.; ELLENS, E.; NAPORA, F.; GILLET, C. L.; GORISSEN, H.; CALDERON, P.; REMACLE, M. D.; JANSSENS DE VAREBEKE, P.; VAN DORSSER, W.; ROBA, J.; Eur.