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Please use this identifier to cite or link to this item: http://hdl.handle.net/1843/72108
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dc.creatorLucas da Silva Santospt_BR
dc.creatorMatheus Fillipe Langanke de Carvalhopt_BR
dc.creatorAna Claudia de Souza Pintopt_BR
dc.creatorAmanda Luisa da Fonsecapt_BR
dc.creatorJulio César Dias Lopespt_BR
dc.creatorFernando de Pilla Varottipt_BR
dc.creatorRossimiriam Pereira de Freitaspt_BR
dc.creatorRosemeire Brondi Alvespt_BR
dc.date.accessioned2024-07-30T13:34:46Z-
dc.date.available2024-07-30T13:34:46Z-
dc.date.issued2021-
dc.citation.volume17pt_BR
dc.citation.issue8pt_BR
dc.citation.spage820pt_BR
dc.citation.epage833pt_BR
dc.identifier.doihttp://dx.doi.org/10.2174/1573406416666200602161047pt_BR
dc.identifier.issn1875-6638pt_BR
dc.identifier.urihttp://hdl.handle.net/1843/72108-
dc.description.resumoBackground: Malaria greatly affects the world health, having caused more than 228 million cases only in 2018. The emergence of drug resistance is one of the main problems in its treatment, demonstrating the need for the development of new antimalarial drugs. Objective: Synthesis and in vitro antiplasmodial evaluation of triazole compounds derived from isocoumarins and a 3,4-dihydroisocoumarin. Methods: The compounds were synthesized in 4 to 6-step reactions with the formation of the triazole ring via the Copper(I)-catalyzed 1,3-dipolar cycloaddition between isocoumarin or 3,4-dihydroisocoumarin azides and terminal alkynes. This key reaction provided compounds with an unprecedented connection of isocoumarin or 3,4-dihydroisocoumarin and the 1,2,3-triazole ring. The products were tested for their antiplasmodial activity against a Plasmodium falciparum chloroquine resistant and sensitive strains (W2 and 3D7, respectively). Results: Thirty-one substances were efficiently obtained by the proposed routes with an overall yield of 25-53%. The active substances in the antiplasmodial test displayed IC50 values ranging from 0.68-2.89μM and 0.85-2.07 μM against W2 and 3D7 strains, respectively. Conclusion: This study demonstrated the great potential of isocoumarin or 3,4-dihydroisocoumarin derivatives because practically all the tested substances were active against Plasmodium falciparum.pt_BR
dc.description.sponsorshipCNPq - Conselho Nacional de Desenvolvimento Científico e Tecnológicopt_BR
dc.description.sponsorshipFAPEMIG - Fundação de Amparo à Pesquisa do Estado de Minas Geraispt_BR
dc.description.sponsorshipCAPES - Coordenação de Aperfeiçoamento de Pessoal de Nível Superiorpt_BR
dc.languageengpt_BR
dc.publisherUniversidade Federal de Minas Geraispt_BR
dc.publisher.countryBrasilpt_BR
dc.publisher.departmentICX - DEPARTAMENTO DE QUÍMICApt_BR
dc.publisher.initialsUFMGpt_BR
dc.relation.ispartofMedicinal Chemistrypt_BR
dc.rightsAcesso Restritopt_BR
dc.subjectIsocoumarinpt_BR
dc.subject3,4-dihydroisocoumarinpt_BR
dc.subject1,2,3-triazolept_BR
dc.subjectAntiplasmodial activitypt_BR
dc.subjectMalariapt_BR
dc.subjectPlasmodium falciparumpt_BR
dc.subject.otherQuímica farmacêuticapt_BR
dc.subject.otherPlasmodium falciparumpt_BR
dc.subject.otherMalárapt_BR
dc.subject.otherSintesept_BR
dc.subject.otherTriazóispt_BR
dc.titleSynthesis of novel 1,2,3-triazole derivatives of isocoumarins and 3,4-dihydroisocoumarin with potential antiplasmodial activity in vitropt_BR
dc.typeArtigo de Periódicopt_BR
dc.url.externahttps://www.eurekaselect.com/article/107051pt_BR
dc.identifier.orcidhttps://orcid.org/0000-0002-5797-4071pt_BR
dc.identifier.orcidhttps://orcid.org/0000-0002-6428-6285pt_BR
dc.identifier.orcidhttps://orcid.org/0000-0002-4592-0367pt_BR
dc.identifier.orcidhttps://orcid.org/0000-0003-1463-850Xpt_BR
dc.identifier.orcidhttps://orcid.org/0000-0002-2939-7780pt_BR
dc.identifier.orcidhttps://orcid.org/0000-0001-6974-3724pt_BR
dc.identifier.orcidhttps://orcid.org/0000-0003-0546-2549pt_BR
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