Please use this identifier to cite or link to this item: http://www.repositorio.ufop.br/handle/123456789/7442
Title: 7-Chloroquinolinotriazoles : synthesis by the azide-alkyne cycloaddition click chemistry, antimalarial activity, cytotoxicity and SAR studies.
Authors: 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
Keywords: Quinolines
Triazoles
Plasmodium falciparum
Issue Date: 2014
Citation: 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.
Abstract: 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
ISSN: 02235234
Appears in Collections:DEFAR - Artigos publicados em periódicos

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