A series of novel bisbenzamidines and bisbenzimidazolines with different li
nkers connecting the aromatic groups was tested in vitro for NMDA receptor
antagonist activity. IC,, values for these compounds ranged from 1.2 to >20
0 mu M. The bisbenzamidine with a homopiperazine ring as the central linker
was found to be the most potent NMDA receptor antagonist among all the pen
tamidine analogues tested so far. (C) 1999 Elsevier Science Ltd. All rights
reserved.