Synthesis of Benzimidazole Derivatives: As Anti‐hypertensive Agents

Abstract

A new series of non peptide angiotensin(A‐II) receptor antagonist has been prepared. This N ‐(biphenyl methyl) imidazoles e.g . 5‐substituted (amino) ‐2‐ phenyl‐1‐(2ʼcarboxy biphenyl‐4‐yl) benzimidazoles differ from the previously reported and related compounds in that they produce a potent hypertensive effect upon oral administration. The earlier series were generally active only when administered intravenously. It has been found that 2’‐position of biphenyl is essential. Only ortho substituted acid possess both high affinity for the AII receptor and oral anti‐hypertensive potency.