Use este identificador para citar ou linkar para este item: http://www.repositorio.ufop.br/handle/123456789/7442
Título: 7-Chloroquinolinotriazoles : synthesis by the azide-alkyne cycloaddition click chemistry, antimalarial activity, cytotoxicity and SAR studies.
Autor(es): Pereira, Guilherme Rocha
Brandão, Geraldo Célio
Arantes, Lucas Micquéias
Oliveira Junior, Haliton Alves de
Paula, Renata Cristina de
Nascimento, Maria Fernanda A. do
Santos, Fábio Mendes dos
Rocha, Ramon Kleber da
Lopes, Julio Cesar Dias
Oliveira, Alaide Braga de
Palavras-chave: Quinolines
Triazoles
Plasmodium falciparum
Data do documento: 2014
Referência: 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.
Resumo: 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
Link para o editor: http://www.sciencedirect.com/science/article/pii/S0223523413007642
ISSN: 02235234
Aparece nas coleções:DEFAR - Artigos publicados em periódicos

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