The antischistosomal activity of oltipraz

E. Bueding, P. Dolan, J. P. Leroy

Research output: Contribution to journalArticle

Abstract

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 languageEnglish (US)
Pages (from-to)293-303
Number of pages11
JournalResearch Communications in Chemical Pathology and Pharmacology
Volume37
Issue number2
StatePublished - Jan 1 1982

ASJC Scopus subject areas

  • Pathology and Forensic Medicine
  • Toxicology
  • Pharmacology
  • Pharmacology, Toxicology and Pharmaceutics(all)

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