Design, synthesis, and evaluation of novelly substituted benzimidazole compounds as angiotensin II receptor antagonists

5-Nitrobenzimidazole derivatives with varying substituents at 2-position have been designed, synthesized, and evaluated for angiotensin II antagonistic activity. A drug–receptor interaction model has been proposed.

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.Figure optionsDownload as PowerPoint slide