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. Leroy et al. (1978) and Leroy and Barreau (1980) have reported that oltipraz (5-(2-pyrazinyl)-4-methyl-1,2-dithiol-3-thione) has antischistosomal activity. This report is dealing with some of the chemotherapeutic properties and structural requirements of this novel antischistosomal compound.
|Original language||English (US)|
|Number of pages||11|
|Journal||Research Communications in Chemical Pathology and Pharmacology|
|State||Published - Jan 1 1982|
ASJC Scopus subject areas
- Pathology and Forensic Medicine
- Pharmacology, Toxicology and Pharmaceutics(all)