Metabolism by Schistosoma mansoni of a new schistosomicide: 2-[(1-methylpropyl)amino]-1-octanethiosulphuric acid.
In order to investigate the mode of action of a new class of schistosomicides, the N-alkylaminoalkanethiosulphuric acids, the [outer 25S] 2-[(1-methylpropyl)amino]-1-octanethiosulphuric acids 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 chromatogrpahy 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.
Penido
M L
ML
Departamento de Bioquímica-Imunologia-ICB, Universidade Federal de Minas Gerais, Brazil.
Nelson
D L
DL
Vieira
L Q
LQ
Watson
D G
DG
Kusel
J R
JR
D000818:Animals; D001345:Autoradiography; D001700:Biomphalaria; D002855:Chromatography, Thin Layer; D004591:Electrophoresis, Polyacrylamide Gel; D005260:Female; D007202:Indicators and Reagents; D007553:Isotope Labeling / Q000379:methods; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D012550:Schistosoma mansoni / Q000378:metabolism*; D012556:Schistosomicides / Q000378:metabolism*; D013462:Sulfur Radioisotopes; D013463:Sulfuric Acid Esters / Q000138:chemical synthesis / Q000378:metabolism* / Q000493:pharmacokinetics; D014018:Tissue Distribution
C095655:2-((1-methylpropyl)amino)-1-octanethiosulfuric acid; D007202:Indicators and Reagents; D012556:Schistosomicides; D013462:Sulfur Radioisotopes; D013463:Sulfuric Acid Esters