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Highly active ozonides selected against drug resistant malaria

dc.contributor.authorLobo, Lis
dc.contributor.authorSousa, Bruno de
dc.contributor.authorCabral, Lília
dc.contributor.authorCristiano, Maria Lurdes Santos
dc.contributor.authorNogueira, Fátima
dc.date.accessioned2017-04-07T15:56:25Z
dc.date.available2017-04-07T15:56:25Z
dc.date.issued2016-07
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.
dc.description.sponsorshipPTDC-QUI-65142-2006
dc.identifier.doi10.1590/0074-02760160077
dc.identifier.issn0074-0276
dc.identifier.otherAUT: MCR00716;
dc.identifier.urihttp://hdl.handle.net/10400.1/9406
dc.language.isoeng
dc.peerreviewedyes
dc.publisherInstituto Oswaldo Cruz, Ministério da Saúde
dc.relationGlobal Health and Tropical Medicine
dc.relation.isbasedonWOS:000380112500005
dc.titleHighly active ozonides selected against drug resistant malaria
dc.typejournal article
dspace.entity.typePublication
oaire.awardTitleGlobal Health and Tropical Medicine
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/6817 - DCRRNI ID/UID%2FMulti%2F04413%2F2013/PT
oaire.citation.endPage453
oaire.citation.issue7
oaire.citation.startPage450
oaire.citation.titleMemórias do Instituto Oswaldo Cruz
oaire.citation.volume111
oaire.fundingStream6817 - DCRRNI ID
person.familyNameCabral
person.familyNameCristiano
person.givenNameLília
person.givenNameMaria de Lurdes
person.identifier.ciencia-id3510-24A8-36B6
person.identifier.ciencia-idE411-6006-5A01
person.identifier.orcid0000-0001-9362-8128
person.identifier.orcid0000-0002-9447-2855
person.identifier.ridM-4279-2013
person.identifier.ridG-2345-2012
person.identifier.scopus-author-id9238724800
project.funder.identifierhttp://doi.org/10.13039/501100001871
project.funder.nameFundação para a Ciência e a Tecnologia
rcaap.rightsopenAccess
rcaap.typearticle
relation.isAuthorOfPublication175a6aa3-9993-480b-9663-ed083a17eedf
relation.isAuthorOfPublicationb16751a6-748e-44b0-9c59-058cbd5b2cc3
relation.isAuthorOfPublication.latestForDiscovery175a6aa3-9993-480b-9663-ed083a17eedf
relation.isProjectOfPublication5a7a17ef-fb7b-49e5-b474-9c4ae38fc4f4
relation.isProjectOfPublication.latestForDiscovery5a7a17ef-fb7b-49e5-b474-9c4ae38fc4f4

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