Please use this identifier to cite or link to this item: https://hdl.handle.net/10316/107437
DC FieldValueLanguage
dc.contributor.authorAlves, Nuno Guerreiro-
dc.contributor.authorBártolo, Inês-
dc.contributor.authorAlves, Américo J. S.-
dc.contributor.authorFontinha, Diana-
dc.contributor.authorFrancisco, Denise-
dc.contributor.authorLopes, Susana M. M.-
dc.contributor.authorSoares, Maria I. L.-
dc.contributor.authorSimões, Carlos J. V.-
dc.contributor.authorPrudêncio, Miguel-
dc.contributor.authorTaveira, Nuno-
dc.contributor.authorPinho e Melo, Teresa M. V. D.-
dc.date.accessioned2023-07-12T08:21:03Z-
dc.date.available2023-07-12T08:21:03Z-
dc.date.issued2021-07-05-
dc.identifier.issn02235234pt
dc.identifier.urihttps://hdl.handle.net/10316/107437-
dc.description.abstractThe synthesis and antimicrobial activity of new spiro-β-lactams is reported. The design of the new molecules was based on the structural modulation of two previously identified lead spiro-penicillanates with dual activity against HIV and Plasmodium. The spiro-β-lactams synthesized were assayed for their in vitro activity against HIV-1, providing relevant structure-activity relationship information. Among the tested compounds, two spirocyclopentenyl-β-lactams were identified as having remarkable nanomolar activity against HIV-1. Additionally, the same molecules showed promising antiplasmodial activity, inhibiting both the hepatic and blood stages of Plasmodium infection.pt
dc.language.isoengpt
dc.publisherElsevierpt
dc.relationSFRH/BD/128910/2017pt
dc.relationPD/BD/135287/2017pt
dc.relationUIDB/04138/2020pt
dc.relationUIDB/00313/2020pt
dc.relationUIDP/00313/2020pt
dc.rightsembargoedAccesspt
dc.rights.urihttp://creativecommons.org/licenses/by-nc-nd/4.0/pt
dc.subject1,3-Dipolar cycloadditionpt
dc.subject2-Butynoatespt
dc.subjectAllenespt
dc.subjectAnti-HIV agentspt
dc.subjectAntiplasmodial agentspt
dc.subjectPhosphane-catalyzed [3+2] annulationspt
dc.subjectSpiro-3H-pyrazole-β-lactamspt
dc.subjectSpiro-penicillanatespt
dc.subjectSpirocyclic compoundspt
dc.subjectSpirocyclopentenyl-β-lactams; β-Lactamspt
dc.subject.meshAnti-HIV Agentspt
dc.subject.meshAntimalarialspt
dc.subject.meshCell Linept
dc.subject.meshCell Survivalpt
dc.subject.meshDrug Designpt
dc.subject.meshHIV-1pt
dc.subject.meshHumanspt
dc.subject.meshLife Cycle Stagespt
dc.subject.meshMolecular Conformationpt
dc.subject.meshPlasmodiumpt
dc.subject.meshSpiro Compoundspt
dc.subject.meshStereoisomerismpt
dc.subject.meshStructure-Activity Relationshippt
dc.subject.meshbeta-Lactamspt
dc.titleSynthesis and structure-activity relationships of new chiral spiro-β-lactams highly active against HIV-1 and Plasmodiumpt
dc.typearticle-
degois.publication.firstPage113439pt
degois.publication.titleEuropean Journal of Medicinal Chemistrypt
dc.peerreviewedyespt
dc.identifier.doi10.1016/j.ejmech.2021.113439pt
degois.publication.volume219pt
dc.date.embargo2023-07-05*
uc.date.periodoEmbargo730pt
item.openairecristypehttp://purl.org/coar/resource_type/c_18cf-
item.grantfulltextopen-
item.openairetypearticle-
item.languageiso639-1en-
item.fulltextCom Texto completo-
item.cerifentitytypePublications-
crisitem.project.grantnoResearch Institute for Medicines - iMed.ULisboa-
crisitem.project.grantnoCoimbra Chemistry Center-
crisitem.project.grantnoCoimbra Chemistry Center-
crisitem.author.researchunitCQC - Coimbra Chemistry Centre-
crisitem.author.researchunitCQC - Coimbra Chemistry Centre-
crisitem.author.researchunitCQC - Coimbra Chemistry Centre-
crisitem.author.researchunitCQC - Coimbra Chemistry Centre-
crisitem.author.researchunitCQC - Coimbra Chemistry Centre-
crisitem.author.parentresearchunitFaculty of Sciences and Technology-
crisitem.author.parentresearchunitFaculty of Sciences and Technology-
crisitem.author.parentresearchunitFaculty of Sciences and Technology-
crisitem.author.parentresearchunitFaculty of Sciences and Technology-
crisitem.author.parentresearchunitFaculty of Sciences and Technology-
crisitem.author.orcid0000-0001-8860-0470-
crisitem.author.orcid0000-0001-5994-9104-
crisitem.author.orcid0000-0003-3256-4954-
Appears in Collections:I&D CQC - Artigos em Revistas Internacionais
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