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Título : | 7-Chloroquinolinotriazoles : synthesis by the azide-alkyne cycloaddition click chemistry, antimalarial activity, cytotoxicity and SAR studies. |
Autor : | Pereira, Guilherme Rocha Brandão, Geraldo Célio Arantes, Lucas Micquéias Oliveira Junior, Haliton Alves de Paula, Renata Cristina de Nascimento, Maria Fernanda Alves do Santos, Fábio Mendes dos Rocha, Ramon Kleber da Lopes, Júlio César Dias Oliveira, Alaíde Braga de |
Palabras clave : | Quinolines Triazoles Plasmodium falciparum |
Fecha de publicación : | 2014 |
Citación : | PEREIRA, 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. |
Resumen : | Twenty-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. |
URI : | http://www.repositorio.ufop.br/handle/123456789/7442 |
metadata.dc.identifier.uri2: | http://www.sciencedirect.com/science/article/pii/S0223523413007642 |
metadata.dc.identifier.doi: | https://doi.org/10.1016/j.ejmech.2013.11.022 |
ISSN : | 0223-5234 |
Aparece en las colecciones: | DEFAR - Artigos publicados em periódicos |
Ficheros en este ítem:
Fichero | Descripción | Tamaño | Formato | |
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ARTIGO_7ChloroquinolinotriazolesSynthesisAzide.pdf Restricted Access | 2,43 MB | Adobe PDF | Visualizar/Abrir |
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