EFFICACY OF AMOSCANATE DERIVATIVES IN EXPERIMENTAL SCHISTOSOMIASIS

Antischistosomal action of some amoseanate (nithiocyaminum) derivatives was tested in screening system of mice injected with Schistosoma japonieum. It was demonstrated that 6 derivatives of Amoscanate coded as S79082, S79083, S80016, S80051, S80063 and S80065 exhibited apparent schistosomicidal effect.Further experimental chemotherapy in mice showed that with S79082, S79083,S80016, S80063, S80065 and amoscanate, at dosages of 250～500 mg/kg/day×1～3, the worm reduction rates were 9.0%, 78.9～99.0%, 98.2～99.6%, 88.9～96.8%, 49.7% and 88.6～97.5%, respectively; while with S80051 at the dosage of 1000 mg/kg/day×3, the rate was 34.2%. With S79083, S80016, S80063 and amoscanate at total dosages of 45～90 mg/kg in 1 to 3-day course, the worm reduction rates were 11.1～30.6%, 58.2～97.3%, 20.3～41.0% and 96.9～99.2%, respectively.When S79083, S80016, S80063 and amoscanate were given to infected rabbits at total dosages of 20, 30 and 60 mg/kg in 2 to 5-day course, worm reduction rates of 91.4～100%, 57.1～100%, 71.8～96.2% and 82.7～100%, respectively, were observed. When the total dosage was reduced to 15 mg/kg, the worm reduction rates of S79083, S80016 and amoscanate were 43.5～69.2%, 15.1～23.5% and 23.4～30.3%, respectively.It appears that the antischistosomal effects of S80016 and amoscanate are comparable in infected mice, and the worm reduction rate of S79083 was higher than that of S80016 and amoscanate in infected rabbits.