Various substituted diphenyl bisamidines were prepared and tested for
antiamoebic activity in Golden hamsters and Wistar rats. Compounds 10
showed in vitro activity at 100 mu g/mL and displayed excellent in viv
o activity against hepatic infection in the hamster. Its in vivo activ
ity against intestinal amoebiasis in the experimental rat was superior
to metronidazole and was comparable to diloxanide furoate. The less p
ronounced in vitro activity, and comparable in vivo activity of compou
nd 10 with respect to the standard drugs, may be due to some of its me
tabolites.