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J Med Chem ; 41(7): 1092-8, 1998 Mar 26.
Article in English | MEDLINE | ID: mdl-9544209

ABSTRACT

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


Subject(s)
Anthelmintics/chemical synthesis , Sulfones/chemical synthesis , Animals , Anthelmintics/chemistry , Anthelmintics/pharmacology , Fasciola hepatica/drug effects , Gerbillinae/parasitology , Haemonchiasis/drug therapy , Haemonchus/drug effects , Muscidae/drug effects , Sheep , Structure-Activity Relationship , Sulfones/pharmacology , Trichostrongylus/drug effects
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