THE ANTI-SCHISTOSOMAL ACTIVITY OF OLTIPRAZ

  • 1 January 1982
    • journal article
    • research article
    • Vol. 37  (2) , 293-303
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 .apprx. 2 mo. 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). 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 et Barreau (1980) reported that oltipraz has antischistosomal activity. Some of the chemotherapeutic properties and structural requirements of this novel antischistosomal compound are here reported.

This publication has 0 references indexed in Scilit: