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Metabolism by Schistosoma mansoni of a new schistosomicide: 2-[(1-methylpropyl)amino]-1-octanethiosulphuric acid

Published online by Cambridge University Press:  06 April 2009

M. L. O. Penido
Affiliation:
Departamento de Bioquímica-Imunologia-ICB, Universidade Federal de Minas Gerais, Belo Horizonte, MG, Brazil
D. L. Nelson
Affiliation:
Departamento de Bioquímica-Imunologia-ICB, Universidade Federal de Minas Gerais, Belo Horizonte, MG, Brazil
L. Q. Vieira
Affiliation:
Departamento de Bioquímica-Imunologia-ICB, Universidade Federal de Minas Gerais, Belo Horizonte, MG, Brazil
D. G. Watson
Affiliation:
Dpartment of Pharmaceutical Sciences, University of Strathclyde, Glasgow, Scotland
J. R. Kusel
Affiliation:
Department of Biochemistry, University of Glasgow, Glasgow, Scotland

Summary

In order to investigate the mode of action of a new class of schistosomicides, the N-alkylaminoalkanethiosulphuric acids, the ‘outer 35S] 2-[(1-methylpropyl)amino]-1-octanethiosulphuric acid was synthesized. Labelling studies of adult Schistosoma mansoni were performed in infected mice and in in vitro incubations. After a single oral dose of the drug to infected mice, 5 metabolites were detected by thin-layer chromatography in organic extracts of male and female adult schistosomes. In vitro studies showed that the same compounds were present in organic extracts obtained from adult male and female worms. One of these metabolites was identified by mass spectroscopy as being the dimeric disulphide derivative of the parent labelled thiosulphuric acid.

Type
Research Article
Copyright
Copyright © Cambridge University Press 1995

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