Balanced AT 1 and AT 2 angiotensin II antagonists. II. Potent 5 α-hydroxyacid imidazolyl biphenyl sulfonylureas

Abstract

Introduction of an α-hydroxyacid moiety in position 5 of the imidazole ring within the imidazolyl biphenyl sulfonyl urea series significantly increased AT 2 binding. Structure activity relationship around this moiety is described and gave rise to balanced AII inhibitors with nanomolar affinity on both AT 1 and AT 2 receptors and with an AT 2 AT 1 ratio of between 0.4 and 3.