%0 Journal Article
%9 ACL : Articles dans des revues avec comité de lecture répertoriées par l'AERES
%A Burguete, A.
%A Estevez, Y.
%A Castillo, D.
%A Gonzalez, G.
%A Villar, R.
%A Solano, B.
%A Vicente, E.
%A Silanes, S. P.
%A Aldana, I.
%A Monge, A.
%A Sauvain, Michel
%A Deharo, Eric
%T Anti-leishmanial and structure-activity relationship of ring substituted 3-phenyl-1-(1,4-di-N-oxide quinoxalin-2-yl)-2-propen-1-one derivatives
%D 2008
%L fdi:010044228
%G ENG
%J Memorias do Instituto Oswaldo Cruz
%@ 0074-0276
%K quinoxaline ; anti-leishmanial ; structure-activity ; Leishmaniasis
%M ISI:000262579800006
%N 8
%P 778-780
%U https://www.documentation.ird.fr/hor/fdi:010044228
%> https://www.documentation.ird.fr/intranet/publi/2009/02/010044228.pdf
%V 103
%W Horizon (IRD)
%X A series of ring substituted 3-phenyl-1-(1,4-di-N-oxide quinoxalin-2-yl)-2-propen-1-one derivatives were synthesized and tested for in vitro leishmanicidal activity against amastigotes of Leishmania amazonensis in axenical cultures and murine infected macrophages. Structure-activity relationships demonstrated the importance of a radical methoxy at position R-3', R-4' and R-5'. (2E)-3-(3,4,5-trimethoxy-phenyl)-1-(3,6,7-trimethyl-1,4-dioxy-quinoxalin -2- yl)-propenone was the most active. Cytotoxicity on macrophages revealed that this product was almost six times more active than toxic.
%$ 052