Diferent classes of antimalarial drugs have been used to treat malaria, but the emergence of resistant strains of Plasmodium these drugs have decreased their efficiency, causing serious public health problem in tropical areas of the world. In this context, we carried out the preparation and antimalarial evaluation of eleven organic compounds: 7-Cl-MAQ, MAQPZ, 7-Cl-MAQPZ, 2-CF3-MAQ, 7-CF3-MAQ, 7-CF3-MAQPZ, 2-CF3-MAQPZ, 8-Cl-MAQ, 7-Cl-BAQ, 7-CF3-BAQ, 8-Cl-BAQ. These were obtained from the same synthetic strategy, via nucleophilic aromatic substitution reaction between 4-chloroquinoline derivatives and diethylenetriamine or 1,2-(aminoethyl) piperazine, reaching moderated to high yields. These compounds were designed based on the molecular structure of chloroquine, a classic antimalarial drug. As for antimalarial activity, only four substances (7-Cl-MAQ, BAQ, 2-CF3-MAQ and 7-CF3-MAQ) were evaluated. Note that the 7-Cl-MAQ was more active in in vitro and in vivo that the BAQ. The same behavior occurred in cytotoxicity assays, with higher values than the BAQ. In in vivo tests, the monoquinolínico derivative (7-Cl-MAQ) significantly reduced parasitemia. Have the 2-CF3-MAQ compounds and 7-CF3-MAQ, were active in vitro, but were inactive in vivo. Keywords: 4-aminoquinolinic derivatives, antimalarials, chloroquine. / Coordenação de Aperfeiçoamento de Pessoal de Nível Superior / Várias classes de antimaláricos têm sido utilizadas para o tratamento da malária, porém o surgimento de cepas de Plasmodium resistentes a esses fármacos têm diminuído suas eficácias, provocando graves problemas de saúde pública em áreas tropicais do mundo. Nesse contexto, realizou-se a preparação, caracterização e avaliação antimalárica de onze derivados aminoquinolínicos: 7-Cl-MAQ, MAQ, MAQPZ, 7-Cl-MAQPZ, 2-CF3-MAQ, 7-CF3-MAQ, 7-CF3-MAQPZ, 2-CF3-MAQPZ, 8-Cl-MAQ, 7-Cl-BAQ, 7-CF3-BAQ, 8-Cl-BAQ. Estes foram obtidos através da mesma estratégia sintética, via reação de substituição nucleofílica aromática, a partir da reação entre derivados de 4-cloroquinolinas com dietilenotriamina ou 1,2-(aminoetil)piperazina, chegando a rendimentos moderados altos a. Estes compostos foram elaborados baseados na estrutura molecular da cloroquina, um clássico fármaco antimalárico. Quanto à atividade antimalárica, apenas quatro substâncias (7-Cl-MAQ, BAQ, 2-CF3-MAQ e 7-CF3-MAQ) foram avaliadas. Vale destacar que a 7-Cl-MAQ foi mais ativa nos testes in vitro e in vivo que a BAQ. O mesmo comportamento ocorreu nos ensaios de citotoxicidade, apresentando valores maiores que a BAQ. Nos testes in vivo, o derivado monoquinolínico (7-Cl-MAQ) reduziu significativamente a parasitemia. Já os compostos 2-CF3-MAQ e 7-CF3-MAQ, mostraram-se ativos in vitro, porém foram inativos in vivo.