Open AccessSynthesis and evaluation of antimalarial activity of curcumin derivatives
Author(s) -
Patrícia Ramos Gomes,
Fábio Balbino Miguel,
Michael Éder de Oliveira,
Vanessa Viana Ferreira,
Daniel Silqueira Martins Guimarães,
Aline Brito de Lima,
Camila de Souza Barbosa,
Mariana Amorim de Oliveira,
Mauro Vieira de Almeida,
Gustavo Henrique Ribeiro Viana,
Mara R.C. Couri,
Fernando de Pilla Varotti
Publication year - 2014
Publication title -
química nova
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.214
H-Index - 73
eISSN - 1678-7064
pISSN - 0100-4042
DOI - 10.5935/0100-4042.20140075
Subject(s) - curcumin , pharmacology , traditional medicine , chemistry , combinatorial chemistry , antimalarial agent , biochemical engineering , malaria , medicine , plasmodium falciparum , engineering , immunology
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