%0 Journal Article
%9 ACL : Articles dans des revues avec comité de lecture répertoriées par l'AERES
%A Marin, A.
%A Lima, L. M.
%A Solano, B.
%A Vicente, E.
%A Silanes, S. P.
%A Maurel, Séverine
%A Sauvain, Michel
%A Aldana, I.
%A Monge, A.
%A Deharo, Eric
%T Antiplasmodial structure-activity relationship of 3-trifluoromethyl-2-arylcarbonylquinoxaline 1,4-di-N-oxide derivatives
%D 2008
%L fdi:010040943
%G ENG
%J Experimental Parasitology
%@ 0014-4894
%M CC:0002529762-0005
%N 1
%P 25-31
%R 10.1016/j.exppara.2007.05.009
%U https://www.documentation.ird.fr/hor/fdi:010040943
%> https://www.documentation.ird.fr/intranet/publi/2008/03/010040943.pdf
%V 118
%W Horizon (IRD)
%X Derivatives of 3-trifluoromethyl-2-arylcarbonylquinoxaline 1,4-di-N-oxide (4b-g, 5b-g, 6a-g) were synthesized and evaluated for their capacity to inhibit the growth of chloroquine-resistant Plasmodium falciparum FCB1 strain in culture. Compound 7-chloro-2-(2-furylcarbonyl)-3-trifluoromethyl-1,4-quinoxaline di-N-oxide (5g) was the most active being almost 5 times more active than chloroquine. It was also 50 times more active against P. falciparum than toxic toward MCF7 cells. Structural characteristics for a quinoxaline to be active were defined: bioisosteric modification of phenyl group by 2-thienyl or 2-furyl subunits, R2 position must be free or occupied by a methyl group and R1 position must be free or occupied by Cl, CH3, OCH3 or CF3.
%$ 052