Abstract Two new benzimidazole derivatives were synthesized and evaluated for their ability to inhibit the binding at the strychnine-insensitive N-methyl-d-aspartate (NMDA)-linked glycine receptor. The most potent one, the 4, 6-dichlorobenzimidazole-2-carboxylic acid 6, was found to have submicromolar affinity for this receptor. The result of its functional test suggests that it acts as an antagonist of the NMDA receptor complex. Thus, this class of ...