Synthesis and AT1 affinity evaluation of benzamidophenyl analogs of known AT1 receptor ligands with similar aromatic skeleton

Abstract

Taking as model compound the amido-derivative 1 described in the literature from Duncia's group as a good AngII antagonist, we have synthesized a new series of compounds (2-7) in which the principal structural variations reside in the inversion of the amidic sequence between the two phenyl ring and/or in the type of heteroaromatic substituent linked to this portion. The new compounds synthesized were evaluated for their AT1 affinity through binding assays carried out on rat liver membranes using [125 I]Sar1,Ile8-angiotensin II as radioligand.