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.