Premium
Synthesis and Antimalarial Properties of New Chloro‐9 H ‐xanthones with an Aminoalkyl Side Chain
Author(s) -
Portela César,
Afonso Carlos M. M.,
Pinto Madalena M. M.,
Lopes Dinora,
Nogueira Fátima,
do Rosário Virgílio
Publication year - 2007
Publication title -
chemistry and biodiversity
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.427
H-Index - 70
eISSN - 1612-1880
pISSN - 1612-1872
DOI - 10.1002/cbdv.200790130
Subject(s) - plasmodium falciparum , chemistry , in vitro , chloroquine , stereochemistry , side chain , protozoa , strain (injury) , biochemistry , malaria , microbiology and biotechnology , organic chemistry , biology , anatomy , immunology , polymer
The synthesis and antimalarial properties of twelve new chlorinated 9 H ‐xanthones, carrying a [2‐(diethylamino)ethyl]amino group in position 1, are reported. All compounds were found to be active towards the chloroquine‐susceptible and chloroquine‐resistant strains 3D7 and Dd2, resp., of the protozoa parasite Plasmodium falciparum. Especially one compound, 6‐chloro‐1‐{[2‐(diethylamino)ethyl]amino}‐9 H ‐xanthen‐9‐one ( 1k ), was found to exhibit significant in vitro activity ( IC 50 =3.9 μ M ) towards the resistant Dd2 strain.