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7-Chloroquinolinotriazoles : synthesis by the azide-alkyne cycloaddition click chemistry, antimalarial activity, cytotoxicity and SAR studies.
(2014) 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
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.