SYNTHESIS AND ENDECTOCIDAL ACTIVITY OF NOVEL 1-(ARYLSULFONYL)-1-[(TRIFLUOROMETHYL) SULFONYL] METHANE DERIVATIVES

We have recently synthesized a series of novel disulfonylmethane compo unds that have shown anthelmintic and insecticidal (endectocidal) acti vity. Several analogues have shown activity against the internal nemat ode Haemonchus contortus. In sheep studies, these analogues have shown 100% control of this internal parasite at a 10 mg/kg rate. In vitro a ctivity against the biting flies, Stomoxys calcitrans and Haematobia i rritans, has been observed at rates as low as 25 and 2.3 ppm, respecti vely. Only marginal activity against the liver fluke Fasciola hepatica and Trichostrongylus colubriformis was seen. Respiratory control inde x values on rat liver mitochondria for this series suggested uncouplin g of oxidative phosphorylation as a mechanism of action. Compound 1 is considered to be a promising agent for treatment of parasitized sheep .