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Highly active ozonides selected against drug resistant malaria

2016-07-01Artigo científico Acesso aberto
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dc.contributor.authorLobo, Lis
dc.contributor.authorde Sousa, Bruno
dc.contributor.authorCabral, Lília I L
dc.contributor.authorCristiano, Maria L S
dc.contributor.authorNogueira, Fátima
dc.contributor.institutionInstituto de Higiene e Medicina Tropical (IHMT)
dc.contributor.institutionVector borne diseases and pathogens (VBD)
dc.contributor.institutionGlobal Health and Tropical Medicine (GHTM)
dc.contributor.pblMemorias Do Instituto Oswaldo Cruz / Instituto Oswaldo Cruz, Ministério da Saúde
dc.date.accessioned2018-05-11T22:06:08Z
dc.date.available2018-05-11T22:06:08Z
dc.date.issued2016-07-01
dc.description.abstractEver increasing multi-drug resistance by Plasmodium falciparum is creating new challenges in malaria chemotherapy. In the absence of licensed vaccines, treatment and prevention of malaria is heavily dependent on drugs. Potency, range of activity, safety, low cost and ease of administration are crucial issues in the design and formulation of antimalarials. We have tested three synthetic ozonides NAC89, LC50 and LCD67 in vitro and in vivo against multidrug resistant Plasmodium. In vitro, LC50 was at least 10 times more efficient inhibiting P. falciparum multidrug resistant Dd2 strain than chloroquine and mefloquine and as efficient as artemisinin (ART), artesunate and dihydroartemisinin. All three ozonides showed high efficacy in clearing parasitaemia in mice, caused by multi-drug resistant Plasmodium chabaudi strains, by subcutaneous administration, demonstrating high efficacy in vivo against ART and artesunate resistant parasites.en
dc.description.versionpublishersversion
dc.description.versionpublished
dc.format.extent4
dc.format.extent233274
dc.identifier.doi10.1590/0074-02760160077
dc.identifier.issn0074-0276
dc.identifier.otherPURE: 2452323
dc.identifier.otherPURE UUID: 24780ee7-d0a6-4a47-a6b8-12b7111ee4d4
dc.identifier.otherScopus: 84976588805
dc.identifier.otherWOS: 000380112500005
dc.identifier.otherPubMed: 27276364
dc.identifier.otherORCID: /0000-0003-0313-0778/work/124583095
dc.identifier.urihttp://www.scopus.com/inward/record.url?scp=84976588805&partnerID=8YFLogxK
dc.identifier.urlhttps://www.scopus.com/pages/publications/84976588805
dc.language.isoeng
dc.peerreviewedyes
dc.subjectDrug resistance
dc.subjectMalaria
dc.subjectOzonides
dc.subjectDrug Discovery
dc.subjectParasitology
dc.subjectInfectious Diseases
dc.subjectSDG 3 - Good Health and Well-being
dc.titleHighly active ozonides selected against drug resistant malariaen
dc.typejournal article
degois.publication.firstPage450
degois.publication.issue7
degois.publication.lastPage453
degois.publication.titleMemórias do Instituto Oswaldo Cruz
degois.publication.volume111
dspace.entity.typePublication
rcaap.rightsopenAccess

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