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Semi-synthetic and synthetic 1,2,4-trioxaquines and 1,2,4-trioxolaquines: synthesis, preliminary SAR and comparison with acridine endoperoxide conjugates

2009Artigo científico Acesso restrito
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dc.contributor.authorAraujo, Nuna C. P.
dc.contributor.authorBarton, Victoria
dc.contributor.authorJones, Michael
dc.contributor.authorStocks, Paul A.
dc.contributor.authorWard, Stephen A.
dc.contributor.authorDavies, Jill
dc.contributor.authorBray, Patrick G.
dc.contributor.authorShone, Alison E.
dc.contributor.authorCristiano, Maria Lurdes Santos
dc.contributor.authorO'Neill, Paul M.
dc.date.accessioned2014-06-07T11:00:48Z
dc.date.available2014-06-07T11:00:48Z
dc.date.issued2009
dc.date.updated2014-06-05T11:06:22Z
dc.description.abstractA novel series of semi-synthetic trioxaquines and synthetic trioxolaquines were prepared, in moderate to good yields. Antimalarial activity was evaluated against both the chloroquine-sensitive 3D7 and resistant K1 strain of Plasmodium falciparum and both series of compounds were shown to be active in the low nanomolar range. For comparison the corresponding 9-amino acridine analogues were also prepared and shown to have low nanomolar activity like their quinoline counterparts.por
dc.identifier.citationAraújo, Nuna C.P.; Barton, Victoria; Jones, Michael; Stocks, Paul A.; Ward, Stephen A.; Davies, Jill; Bray, Patrick G.; Shone, Alison E.; Cristiano, Maria L.S.; O’Neill, Paul M. Semi-synthetic and synthetic 1,2,4-trioxaquines and 1,2,4-trioxolaquines: synthesis, preliminary SAR and comparison with acridine endoperoxide conjugates, Bioorganic & Medicinal Chemistry Letters, 19, 7, 2038-2043, 2009.por
dc.identifier.doihttp://dx.doi.org/10.1016/j.bmcl.2009.02.013
dc.identifier.issn0960-894X
dc.identifier.otherAUT: MCR00716;
dc.identifier.urihttp://hdl.handle.net/10400.1/4242
dc.language.isoengpor
dc.peerreviewedyespor
dc.publisherElsevierpor
dc.subjectAntimalarialpor
dc.subjectResistancepor
dc.subjectPlasmodium falciparumpor
dc.subjectDrug-hybridpor
dc.titleSemi-synthetic and synthetic 1,2,4-trioxaquines and 1,2,4-trioxolaquines: synthesis, preliminary SAR and comparison with acridine endoperoxide conjugatespor
dc.typejournal article
dspace.entity.typePublication
oaire.citation.endPage2043por
oaire.citation.issue7por
oaire.citation.startPage2038por
oaire.citation.titleBioorganic & Medicinal Chemistry Letterspor
oaire.citation.volume19por
person.familyNameAraujo
person.familyNameCristiano
person.givenNameNuna
person.givenNameMaria de Lurdes
person.identifier.ciencia-idE411-6006-5A01
person.identifier.orcid0000-0002-7602-0150
person.identifier.orcid0000-0002-9447-2855
person.identifier.ridN-8531-2013
person.identifier.ridG-2345-2012
person.identifier.scopus-author-id9238724800
rcaap.rightsrestrictedAccesspor
rcaap.typearticlepor
relation.isAuthorOfPublication3423e71b-934d-4da7-9c81-4e56c7930252
relation.isAuthorOfPublicationb16751a6-748e-44b0-9c59-058cbd5b2cc3
relation.isAuthorOfPublication.latestForDiscovery3423e71b-934d-4da7-9c81-4e56c7930252

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