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Praziquantel for Schistosomiasis: Single-Drug Metabolism Revisited, Mode of Action, and Resistance

2017-05Journal article Restricted access
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dc.contributor.authorVale, Nuno
dc.contributor.authorGouveia, Maria João
dc.contributor.authorRinaldi, Gabriel
dc.contributor.authorBrindley, Paul J.
dc.contributor.authorGärtner, Fátima
dc.contributor.authorCorreia da Costa, José M.
dc.date.accessioned2018-03-22T19:03:18Z
dc.date.available2018-03-22T19:03:18Z
dc.date.issued2017-05
dc.description.abstractSchistosomiasis, a major neglected tropical disease, affects more than 250 million people worldwide. Treatment of schistosomiasis has relied on the anthelmintic drug praziquantel (PZQ) for more than a generation. PZQ is the drug of choice for the treatment of schistosomiasis; it is effective against all major forms of schistosomiasis, although it is less active against juvenile than mature parasites. A pyrazino-isoquinoline derivative, PZQ is not considered to be toxic and generally causes few or transient, mild side effects. Increasingly, mass drug administration targeting populations in sub-Saharan Africa where schistosomiasis is endemic has led to the appearance of reduced efficacy of PZQ, which portends the selection of drug-resistant forms of these pathogens. The synthesis of improved derivatives of PZQ is attracting attention, e.g., in the (i) synthesis of drug analogues, (ii) rational design of pharmacophores, and (iii) discovery of new compounds from large-scale screening programs. This article reviews reports from the 1970s to the present on the metabolism and mechanism of action of PZQ and its derivatives against schistosomes.pt_PT
dc.description.sponsorshipWe acknowledge support from the Fundação para a Ciência e Tecnologia (FCT, Portugal) and FEDER (European Union) through UID/MULTI/04378/2013 and project Minireview Antimicrobial Agents and Chemotherapy May 2017 Volume 61 Issue 5 e02582-16 aac.asm.org 12 Downloaded from http://aac.asm.org/ on March 12, 2018 by B-ON FCCN TRIAL grant IF/00092/2014 and from award R01CA164719 from the National Cancer Institute (NCI), National Institutes of Health (NIH). We thank FCT for the IF2014 position (N.V.) and Pest-OE/AGR/UI0211/2011 and Strategic Project UI211 (J.M.C.C).pt_PT
dc.description.versioninfo:eu-repo/semantics/publishedVersionpt_PT
dc.identifier.citationAntimicrob Agents Chemother. 2017 Apr 24;61(5). pii: e02582-16. doi: 10.1128/AAC.02582-16. Print 2017 May.pt_PT
dc.identifier.doi10.1128/AAC.02582-16pt_PT
dc.identifier.issn0066-4804
dc.identifier.urihttp://hdl.handle.net/10400.18/5457
dc.language.isoengpt_PT
dc.peerreviewedyespt_PT
dc.publisherAmerican Society for Microbiologypt_PT
dc.relation.publisherversionhttp://aac.asm.org/content/61/5/e02582-16.longpt_PT
dc.subjectAfrica South of the Saharapt_PT
dc.subjectAnimalspt_PT
dc.subjectDrug Resistancept_PT
dc.subjectHumanspt_PT
dc.subjectSchistosomapt_PT
dc.subjectSchistosomiasispt_PT
dc.subjectSchistosomicidespt_PT
dc.subjectPraziquantelpt_PT
dc.subjectInfecções Sistémicas e Zoonosespt_PT
dc.subjectResistência aos Antimicrobianospt_PT
dc.titlePraziquantel for Schistosomiasis: Single-Drug Metabolism Revisited, Mode of Action, and Resistancept_PT
dc.typejournal article
dspace.entity.typePublication
oaire.citation.issue5pt_PT
oaire.citation.startPagepii: e02582-16pt_PT
oaire.citation.titleAntimicrobial Agents and Chemotherapypt_PT
oaire.citation.volume61pt_PT
rcaap.rightsopenAccesspt_PT
rcaap.typearticlept_PT

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