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4,9‐Diaminoacridines and 4‐Aminoacridines as dual‐stage antiplasmodial hits

2020Journal article Restricted access
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dc.contributor.authorFonte, Mélanie
dc.contributor.authorTassi, Natália
dc.contributor.authorFontinha, Diana
dc.contributor.authorBouzón‐Arnáiz, Inés
dc.contributor.authorFerraz, Ricardo
dc.contributor.authorAraújo, Maria J.
dc.contributor.authorFernàndez‐Busquets, Xavier
dc.contributor.authorPrudêncio, Miguel
dc.contributor.authorGomes, Paula
dc.contributor.authorTeixeira, Cátia
dc.date.accessioned2022-09-07T10:46:02Z
dc.date.available2022-09-07T10:46:02Z
dc.date.issued2020
dc.description© 2020 Wiley-VCH GmbHpt_PT
dc.description.abstractMulti-stage drugs have been prioritized in antimalarial drug discovery, as targeting more than one process in the Plasmodium life cycle is likely to increase efficiency, while decreasing the chances of emergence of resistance by the parasite. Herein, we disclose two novel acridine-based families of compounds that combine the structural features of primaquine and chloroquine. Compounds prepared and studied thus far retained the in vitro activity displayed by the parent drugs against the erythrocytic stages of chloroquine-sensitive and -resistant Plasmodium falciparum strains, and against the hepatic stages of Plasmodium berghei, hence acting as dual-stage antiplasmodial hits.pt_PT
dc.description.sponsorshipThis work was developed within scope of projects UIDB/50006/2020, PTDC/BTM-SAL/29786/2017 and PTDC/SAU-INF/29550/2017, funded by Fundação para a Ciência e Tecnologia (FCT, Portugal). X.F.-B. was funded by i) The Spanish Ministry of Science, Innovation and Universities (http://www.ciencia.gob.es/), grant no. RTI2018-094579-B−I00 (which included FEDER funds), and ii) Generalitat de Catalunya, Spain (http://agaur.gencat.cat/), grant no. 2017-SGR-908. M.F. thanks FCT for doctoral grant SFRH/BD/147345/2019.pt_PT
dc.description.versioninfo:eu-repo/semantics/publishedVersionpt_PT
dc.identifier.citationChemMedChem. 2021 Mar 3;16(5):788-792pt_PT
dc.identifier.doi10.1002/cmdc.202000740pt_PT
dc.identifier.eissn1860-7187
dc.identifier.issn1860-7179
dc.identifier.urihttp://hdl.handle.net/10451/54341
dc.language.isoengpt_PT
dc.peerreviewedyespt_PT
dc.publisherWileypt_PT
dc.relationAssociated Laboratory for Green Chemistry - Clean Technologies and Processes
dc.relationA small couple against the big three
dc.relationEnabling strategies for enhanced whole-sporozoite malaria vaccines
dc.relationMISTRAL – novel 4-amino- and 4,9-diamino-acridines as MultI-STage antimalaRiALs
dc.relation.publisherversionhttps://chemistry-europe.onlinelibrary.wiley.com/journal/18607187pt_PT
dc.subjectPlasmodiumpt_PT
dc.subjectAcridinespt_PT
dc.subjectAntimalarial activitypt_PT
dc.subjectBlood-stagept_PT
dc.subjectLiver-stagept_PT
dc.subjectMalariapt_PT
dc.subjectSynthesispt_PT
dc.title4,9‐Diaminoacridines and 4‐Aminoacridines as dual‐stage antiplasmodial hitspt_PT
dc.typejournal article
dspace.entity.typePublication
oaire.awardTitleAssociated Laboratory for Green Chemistry - Clean Technologies and Processes
oaire.awardTitleA small couple against the big three
oaire.awardTitleEnabling strategies for enhanced whole-sporozoite malaria vaccines
oaire.awardTitleMISTRAL – novel 4-amino- and 4,9-diamino-acridines as MultI-STage antimalaRiALs
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/6817 - DCRRNI ID/UIDB%2F50006%2F2020/PT
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/3599-PPCDT/PTDC%2FBTM-SAL%2F29786%2F2017/PT
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/9471 - RIDTI/PTDC%2FSAU-INF%2F29550%2F2017/PT
oaire.awardURIinfo:eu-repo/grantAgreement/FCT/OE/SFRH%2FBD%2F147345%2F2019/PT
oaire.citation.endPage792pt_PT
oaire.citation.issue5pt_PT
oaire.citation.startPage788pt_PT
oaire.citation.titleChemMedChempt_PT
oaire.citation.volume16pt_PT
oaire.fundingStream6817 - DCRRNI ID
oaire.fundingStream3599-PPCDT
oaire.fundingStream9471 - RIDTI
oaire.fundingStreamOE
person.familyNameFontinha
person.familyNamePrudêncio
person.givenNameDiana
person.givenNameMiguel
person.identifierhttps://scholar.google.pt/citations?user=zduN6wsAAAAJ&hl=pt-PT&oi=ao
person.identifier.ciencia-id6A17-C404-F33B
person.identifier.ciencia-id5511-16ED-48E0
person.identifier.orcid0000-0002-0046-648X
person.identifier.orcid0000-0003-1746-6029
person.identifier.scopus-author-id6603561872
project.funder.identifierhttp://doi.org/10.13039/501100001871
project.funder.identifierhttp://doi.org/10.13039/501100001871
project.funder.identifierhttp://doi.org/10.13039/501100001871
project.funder.identifierhttp://doi.org/10.13039/501100001871
project.funder.nameFundação para a Ciência e a Tecnologia
project.funder.nameFundação para a Ciência e a Tecnologia
project.funder.nameFundação para a Ciência e a Tecnologia
project.funder.nameFundação para a Ciência e a Tecnologia
rcaap.rightsrestrictedAccesspt_PT
rcaap.typearticlept_PT
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