Novel bisbenzamidines and bisbenzimidazolines as noncompetitive NMDA receptor antagonists

A series of novel bisbenzamidines and bisbenzimidazolines with different linker connecting the aromatic groups was tested in vitro for NMDA receptor antagonist activity. IC50 values for these compounds ranged from 1.2 to>200 μM. The bisbenzamidine with a homopiperazine ring as the central linker was found to be the most potent NMDA receptor antagonist among all the pentamidine analogues tested so far.