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Synthesis and Antileishmanial Activity of 1,2,4,5-Tetraoxanes against Leishmania donovani

2020Journal article Open access
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dc.contributor.authorCabral, Lília
dc.contributor.authorPomel, Sébastien
dc.contributor.authorCojean, Sandrine
dc.contributor.authorAmado, Patrícia
dc.contributor.authorLoiseau, Philippe M.
dc.contributor.authorCristiano, Maria De Lurdes
dc.date.accessioned2020-03-18T14:28:49Z
dc.date.available2020-03-18T14:28:49Z
dc.date.issued2020
dc.description.abstractA chemically diverse range of novel tetraoxanes was synthesized and evaluated in vitro against intramacrophage amastigote forms of Leishmania donovani. All 15 tested tetraoxanes displayed activity, with IC50 values ranging from 2 to 45 µm. The most active tetraoxane, compound LC140, exhibited an IC50 value of 2.52 ± 0.65 µm on L. donovani intramacrophage amastigotes, with a selectivity index of 13.5. This compound reduced the liver parasite burden of L. donovani-infected mice by 37% after an intraperitoneal treatment at 10 mg/kg/day for five consecutive days, whereas miltefosine, an antileishmanial drug in use, reduced it by 66%. These results provide a relevant basis for the development of further tetraoxanes as effective, safe, and cheap drugs against leishmaniasis.pt_PT
dc.description.sponsorshipThis research was funded by Fundação para a Ciência e a Tecnologia (FCT), and FEDER/COMPETE 2020-UE, through projects UID/Multi/04326/2019 (Centre of Marine Sciences-CCMAR) and PTDC/MAR-BIO/4132/2014.pt_PT
dc.description.versioninfo:eu-repo/semantics/publishedVersionpt_PT
dc.identifier.doi10.3390/molecules25030465pt_PT
dc.identifier.issn1420-3049
dc.identifier.urihttp://hdl.handle.net/10400.1/13609
dc.language.isoengpt_PT
dc.peerreviewedyespt_PT
dc.subjectLeishmaniasispt_PT
dc.subjectAntileishmanial chemotherapypt_PT
dc.subjectPeroxide-derived antimalarialspt_PT
dc.subjectAntimalarials re-purposingpt_PT
dc.subjectTetraoxanespt_PT
dc.titleSynthesis and Antileishmanial Activity of 1,2,4,5-Tetraoxanes against Leishmania donovanipt_PT
dc.typejournal article
dspace.entity.typePublication
oaire.citation.issue3pt_PT
oaire.citation.startPage465pt_PT
oaire.citation.titleMoleculespt_PT
oaire.citation.volume25pt_PT
person.familyNameCabral
person.familyNameMenalha Amado
person.familyNameCristiano
person.givenNameLília
person.givenNamePatrícia Sofia
person.givenNameMaria de Lurdes
person.identifier.ciencia-id3510-24A8-36B6
person.identifier.ciencia-id8617-A360-B70A
person.identifier.ciencia-idE411-6006-5A01
person.identifier.orcid0000-0001-9362-8128
person.identifier.orcid0000-0002-7307-9210
person.identifier.orcid0000-0002-9447-2855
person.identifier.ridM-4279-2013
person.identifier.ridG-2345-2012
person.identifier.scopus-author-id9238724800
rcaap.rightsopenAccesspt_PT
rcaap.typearticlept_PT
relation.isAuthorOfPublication175a6aa3-9993-480b-9663-ed083a17eedf
relation.isAuthorOfPublication5b28f1eb-1d56-4094-8242-2d1163618e5f
relation.isAuthorOfPublicationb16751a6-748e-44b0-9c59-058cbd5b2cc3
relation.isAuthorOfPublication.latestForDiscovery5b28f1eb-1d56-4094-8242-2d1163618e5f

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