7-Chloroquinolinotriazoles : synthesis by the azide-alkyne cycloaddition click chemistry, antimalarial activity, cytotoxicity and SAR studies.

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dc.contributor.authorPereira, Guilherme Rocha
dc.contributor.authorBrandão, Geraldo Célio
dc.contributor.authorArantes, Lucas Micquéias
dc.contributor.authorOliveira Junior, Haliton Alves de
dc.contributor.authorPaula, Renata Cristina de
dc.contributor.authorNascimento, Maria Fernanda Alves do
dc.contributor.authorSantos, Fábio Mendes dos
dc.contributor.authorRocha, Ramon Kleber da
dc.contributor.authorLopes, Júlio César Dias
dc.contributor.authorOliveira, Alaíde Braga de
dc.date.accessioned2017-03-23T17:05:32Z
dc.date.available2017-03-23T17:05:32Z
dc.date.issued2014
dc.description.abstractTwenty-seven 7-chloroquinolinotriazole derivatives with different substituents in the triazole moiety were synthesized via copper-catalyzed cycloaddition (CuAAC) click chemistry between 4-azido-7- chloroquinoline and several alkynes. All the synthetic compounds were evaluated for their in vitro activity against Plasmodium falciparum (W2) and cytotoxicity to Hep G2A16 cells. All the products disclosed low cytotoxicity (CC50 > 100 mM) and five of them have shown moderate antimalarial activity (IC50 from 9.6 to 40.9 mM). As chloroquine analogs it was expected that these compounds might inhibit the heme polymerization and SAR studies were performed aiming to explain their antimalarial profile. New structural variations can be designed on the basis of the results obtained.pt_BR
dc.identifier.citationPEREIRA, G. R. et al. 7-Chloroquinolinotriazoles: synthesis by the azide-alkyne cycloaddition click chemistry, antimalarial activity, cytotoxicity and SAR studies. European Journal of Medicinal Chemistry, v. 73, p. 295-309, 2014. Disponível em: <http://www.sciencedirect.com/science/article/pii/S0223523413007642>. Acesso em: 10 jan. 2017.pt_BR
dc.identifier.doihttps://doi.org/10.1016/j.ejmech.2013.11.022
dc.identifier.issn0223-5234
dc.identifier.urihttp://www.repositorio.ufop.br/handle/123456789/7442
dc.identifier.uri2http://www.sciencedirect.com/science/article/pii/S0223523413007642pt_BR
dc.language.isoen_USpt_BR
dc.rightsrestritopt_BR
dc.rights.uriAn error occurred getting the license - uri.*
dc.subjectQuinolinespt_BR
dc.subjectTriazolespt_BR
dc.subjectPlasmodium falciparumpt_BR
dc.title7-Chloroquinolinotriazoles : synthesis by the azide-alkyne cycloaddition click chemistry, antimalarial activity, cytotoxicity and SAR studies.pt_BR
dc.typeArtigo publicado em periodicopt_BR
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