Síntese e avaliação da atividade antimalárica de compostos derivados da curcumina

Gomes, Patrícia Ramos, Miguel, Fábio Balbino, Oliveira, Michael Éder de, Ferreira, Vanessa Viana, Guimarães, Daniel Silqueira Martins, Lima, Aline Brito de, Barbosa, Camila de Souza, Oliveira, Mariana Amorim de, Almeida, Mauro Vieira de, Viana, Gustavo Henrique Ribeiro, Couri, Mara Rubia Costa, Varotti, Fernando de Pilla

Síntese e avaliação da atividade antimalárica de compostos derivados da curcumina

AUTOR(ES)

Gomes, Patrícia Ramos, Miguel, Fábio Balbino, Oliveira, Michael Éder de, Ferreira, Vanessa Viana, Guimarães, Daniel Silqueira Martins, Lima, Aline Brito de, Barbosa, Camila de Souza, Oliveira, Mariana Amorim de, Almeida, Mauro Vieira de, Viana, Gustavo Henrique Ribeiro, Couri, Mara Rubia Costa, Varotti, Fernando de Pilla

FONTE

Quím. Nova

DATA DE PUBLICAÇÃO

2014-06

RESUMO

One of the main challenges in the development of new antimalarial drugs is to achieve a viable lead candidate with good pharmacokinetic properties. Curcumin has a broad range of biological activities, including antimalarial activity. Herein, we report the antimalarial activity of six curcumin derivatives (6-12) and an initial analysis of their pharmacokinetic properties. Five compounds have demonstrated potent activity against the P. falciparum in vitro (IC50 values ranging from 1.7 to 15.2 µg mL-1), with moderate or low cytotoxicity against the HeLa cell line. The substitution of the carbonyl group in 6 by a 2,4-dinitrophenylhydrazone group (to afford 11) increases the Selective Index. These preliminary results indicate curcumin derivatives as potential antimalarial compounds.