THE ANTISCHISTOSOMAL ACTIVITY OF A CHLOROINDAZOLE ANALOG OF HYCANTHONE IN MICE INFECTED WITH SCHISTOSOMA MANSONI

¹ Department of Pathobiology, School of hygiene and Public Health; Department of Pharmacology and Experimental Therapeutics, School of Medicine, The Johns Hopkins University, Baltimore, Maryland; Department of Medical Zoology, Walter Reed Army Institute of Research, Washington, D.C.

When tested against six different strains of Schistosoma mansoni, a 6-chlorobenzothia-pyranoindazole analog of hycanthone was found to have antischistosomal activity in mice equal to that of hyeanthone. A hycanthone-resistant strain of S. mansoni proved to be cross-resistant to the analog. Both compounds had similar biochemical effects on schistosomes. The acute toxicity of the analog for mice was lower than that of hycanthone. Since, in contrast to hycanthone, the 6-chloroindazole analog has been shown to have only weak mutagenic activity and to have no detectable teratogenic, malignant cell transforming and hepatotoxic effects, it appears that, within this group of thioxanthenes, mutagenic and other undesirable properties can he dissociated from schistosomicidal activity by suitable structural modifications.

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				P. B. Hulbert, P. E. Hartman, and E. Bueding Hycanthone Analogs: Dissociation of Mutagenic Effects from Antischistosomal Effects Science, November 15, 1974; 186(4164): 647 - 648. [Abstract] [PDF]