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New 4-aminoacridine-cinnamic acid conjugates as multi-stage antimalarial hits

2022-11Conference object Open access
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dc.contributor.authorFonte, Mélanie
dc.contributor.authorFontinha, Diana
dc.contributor.authorMoita, Diana
dc.contributor.authorPrades, Omar
dc.contributor.authorPadilla, Yunuen
dc.contributor.authorFerraz, Ricardo
dc.contributor.authorFernàndez-Busquets, Xavier
dc.contributor.authorPrudêncio, Miguel
dc.contributor.authorGomes, Paula
dc.contributor.authorTeixeira, Cátia
dc.date.accessioned2025-01-07T17:21:03Z
dc.date.available2025-01-07T17:21:03Z
dc.date.issued2022-11
dc.description.abstractThe eradication of malaria remains to be achieved, mainly due to the continued spread of drugresistant parasites. To overcome this, multi-stage drugs have been prioritized in antimalarial drug discovery, since targeting more than one process in the Plasmodium’s life cycle may increase efficiency, while decreasing the chances of resistance emergence by the parasite. Quinacrine (QN) was the first synthetic antiplasmodial drug active against blood forms of the Plasmodium parasite but was rapidly superseded by chloroquine (CQ) which has greater safety, efficiency, and bioavailability. Analysing the QN structure, its acridine core is a fusion between the heterocycle core of CQ and primaquine (PQ), another antiplasmodial drug active against liver forms of the parasite, and able to block malaria transmission. A new family of QN derivatives reported by us, 4-aminoacridines, corresponding to the merge of CQ core and PQ, showed moderate dual-stage antimalarial activity. We have now developed a second generation of 4-aminoacridines (Fig.1) through their conjugation to cinnamic acids (CA) of natural origin that have been reported to enhance antimalarial activity when conjugated to antimalarials. In this communication, we will present the chemical synthesis of this new family of N-cinnamoyl-4-aminoacridines and the in vitro assessment or their activity against a) liver stages of P. berghei, b) erythrocytic forms of P. falciparum, and c) early and mature gametocytes of P. falciparum. Results demonstrate that the conjugation of the CA moiety to the 4-aminoacridine core delivers new compounds with enhanced in vitro activity against all three stages of the malaria parasite lifecycle inside mammalian hosts.pt_PT
dc.description.versioninfo:eu-repo/semantics/publishedVersionpt_PT
dc.identifier.citationFonte, M., Fontinha, D., Moita, D., Prades, O., Padilla, Y., Ferraz, R., Fernàndez-Busquets, X., Prudêncio, M., Gomes, P., & Teixeira, C. (2022). New 4-aminoacridine-cinnamic acid conjugates as multi-stage antimalarial hits. Libro de resúmenes del XXVI Encontro Internacional Galego‐Portugués de Química., 553. https://www.colquiga.org/_files/ugd/398543_55f54cb41f0849d2b908563d15c992b5.pdfpt_PT
dc.identifier.isbn978-84-09-45895-0
dc.identifier.urihttp://hdl.handle.net/10400.22/27030
dc.language.isoengpt_PT
dc.publisherColegio Oficial de Químicos de Galiciapt_PT
dc.relationThanks are further due to FCT/MCTES for the financial support to the LAQV-REQUIMTE research unit through project UIDB/50006/2020, and for the doctoral grant SFRH/BD/147345/2019 to MF.pt_PT
dc.relation.publisherversionhttps://www.colquiga.org/_files/ugd/398543_55f54cb41f0849d2b908563d15c992b5.pdfpt_PT
dc.subjectMalariapt_PT
dc.titleNew 4-aminoacridine-cinnamic acid conjugates as multi-stage antimalarial hitspt_PT
dc.typeconference object
dspace.entity.typePublication
oaire.citation.conferencePlaceSantiago de Compostelapt_PT
oaire.citation.startPage553pt_PT
oaire.citation.titleLibro de resúmenes del XXVI Encontro Internacional Galego‐Portugués de Química.pt_PT
person.familyNameFerraz
person.givenNameRicardo
person.identifier.ciencia-id001E-71CE-F92D
person.identifier.orcid0000-0002-1761-117X
person.identifier.ridG-5639-2011
person.identifier.scopus-author-id24464208500
rcaap.rightsopenAccesspt_PT
rcaap.typeconferenceObjectpt_PT
relation.isAuthorOfPublicationa5a8faa7-12a5-4b1c-bced-44c895677397
relation.isAuthorOfPublication.latestForDiscoverya5a8faa7-12a5-4b1c-bced-44c895677397

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