SYNTHESIS OF DIPHENYL BISAMIDINES AS POTENTIAL AMEBICIDES

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.