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Ferrocenyl, Ruthenocenyl, and Benzyl Oxamniquine Derivatives with Cross-Species Activity against Schistosoma mansoni and Schistosoma haematobium.
ACS Infect Dis
September 2017
Chimie ParisTech, PSL Research University, Laboratory for Inorganic Chemical Biology , F-75005 Paris, France.
Schistosomiasis is a parasitic disease that affects more than 250 million people annually, mostly children in poor, tropical, rural areas. Only one treatment (praziquantel) is available, putting control efforts at risk should resistance occur. In pursuit of treatment alternatives, we derivatized an old antischistosomal agent, oxamniquine (OXA).
View Article and Find Full Text PDFAssociation of oxamniquine praziquantel and clonazepam in experimental Schistosomiasis mansoni.
Mem Inst Oswaldo Cruz
December 2008
Laboratório de Esquistossomose, Instituto René Rachou-Fiocruz, Belo Horizonte, MG, Brasil.
The antischistosomal activity of clonazepam, when administered alone or in association with oxamniquine and praziquantel, was experimentally evaluated in mice infected with Schistosoma mansoni. The animals were treated 45 days post-infection with a single dose, by oral route, according to three treatment schedules: clonazepam 25 mg/kg and sacrificed 15 min, 1h or 4 h after treatment; clonazepam 1.0, 2.
View Article and Find Full Text PDFA case of Schistosoma mansoni infection treated during the prepatent period.
Nat Clin Pract Gastroenterol Hepatol
February 2008
Laboratory of Schistosomiasis at Research Center René Rachou, Fiocruz, Brazil.
Background: A 40-year-old female laboratory technician accidentally came into contact with water that contained snails shedding Schistosoma mansoni cercariae while she was maintaining an aquarium. Several minutes after exposure to the contaminated water, she experienced severe itching in the area of exposure, and several papules were observed.
Investigations: Taking of medical history to provide evidence of accidental contact with water contaminated with S.
Spectrofluorimetric determination of oxamniquine in dosage forms and spiked human plasma through derivatization with 1-dimethylaminonaphthalene-5-sulphonyl chloride.
J Fluoresc
March 2008
Department of Analytical Chemistry, Faculty of Pharmacy, University of Mansoura, Mansoura, Egypt.
A sensitive, simple and selective spectrofluorimetric method was developed for the determination of oxamniquine (OXM) in pharmaceutical formulations and biological fluids. The method is based on the reaction between the drug and 1-dimethylaminonaphthalene-5-sulphonyl chloride (dansyl chloride) in presence of 0.5 M sodium carbonate (pH 10) to yield a highly fluorescent derivative that is measured at 445 nm after excitation at 335 nm.
View Article and Find Full Text PDFThe schistosome enzyme that activates oxamniquine has the characteristics of a sulfotransferase.
Mem Inst Oswaldo Cruz
September 2006
Institute of Cell Biology, CNR, 31 via Ramarini, 00016 Monterotondo, Rome, Italy.
Available evidence suggests that the antischistosomal drug oxamniquine is converted to a reactive ester by a schistosome enzyme that is missing in drug-resistant parasites. This study presents data supporting the idea that the active ester is a sulfate and the activating enzyme is a sulfotransferase. Evidence comes from the fact that the parasite extract loses its activating capability upon dialysis, implying the requirement of some dialyzable cofactor.
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