The antischistosomal activity of oltipraz.
Administration of a single oral dose of oltipraz (5-(2-pyrazinyl)-4 methyl-1,2 dithiol-3-thione) to mice infected with Schistosoma mansoni resulted in the elimination of the parasites. Oltipraz is a slow-acting drug and approximately 2 months are required until its full schistosomicidal effect becomes evident. One of the earliest effects of the drug is a reduction of the glutathione stores of the worms. The antischistosomal activity of oltipraz is lowered when drug metabolism is stimulated by pretreatment with phenobarbital or butyl-hydroxyanisole (BHA). By contrast, administration of L-cysteine is synergistic with the antischistosomal effect of oltipraz. Evaluation of a limited number of oltipraz analogs revealed among dithiolthiones rather stringent structural requirements for antischistosomal activity.
D000818:Animals; D004790:Enzyme Induction / Q000187:drug effects; D005260:Female; D005978:Glutathione / Q000378:metabolism; D051379:Mice; D011719:Pyrazines / Q000494:pharmacology*; D012550:Schistosoma mansoni / Q000378:metabolism; D012552:Schistosomiasis / Q000188:drug therapy / Q000469:parasitology; D012556:Schistosomicides / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013871:Thiones; D013876:Thiophenes; D013997:Time Factors
D011719:Pyrazines; D012556:Schistosomicides; D013871:Thiones; D013876:Thiophenes; C026209:oltipraz; D005978:Glutathione