5-Nitrobenzimidazole coupled through a methylene linker to biphenyl carboxylic acid has been synthesized and evaluated for angiotensin II antagonism activity. On the basis of their higher activity over standard compounds, a binding profile for benzimidazole-based compounds has been proposed. Alkyl group at 2-position has also been optimized with respect to 5-substituent. ... Angiotensin II (Ang II) receptor antagonists are widely accepted as novel ...