Abstract
‘MIRACIL D’ (‘Lucanthone’, I)1 is an orally active schistosomicidal drug which is of limited value in the treatment of human S. haematobium and S. mansoni infections2. For a variety of reasons it was thought that the effects of this agent were mediated through a therapeutically more active metabolite. A number of abortive attempts have been made to identify and isolate this substance. The latest and most thorough investigation was carried out by Strufe3, who found that the drug underwent extensive metabolic transformation in all species studied. The major urinary metabolite in the mouse proved to be the sulphone (II), while the monkey furnished the sulphoxide (III) and man excreted a ‘chromopeptide’, a complex of III with polypeptide. It was concluded that none of the above ‘Miracil D’ derivatives qualified as the elusive active agent.
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References
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Analyses for all new compounds were satisfactory. These were carried out under the supervision of Mr. K. D. Fleischer. Nuclear magnetic resonance and infra-red spectra were performed under the supervision of Dr. F. C. Nachod. We thank Drs. H. P. Drobeck and F. J. Rosenberg for their assistance.
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Kikuth, W., and Gönnert, R., Ann. Trop. Med. Parasit., 42, 256 (1948).
Gönnert, R., Bull. World Health Org., 25, 702 (1961).
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ROSI, D., PERUZZOTTI, G., DENNIS, E. et al. A New, Active Metabolite of ‘Miracil D’. Nature 208, 1005–1006 (1965). https://doi.org/10.1038/2081005a0
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DOI: https://doi.org/10.1038/2081005a0
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