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
AUTOR(ES)
Burguete, Asunción, Estevez, Yannick, Castillo, Denis, González, Germán, Villar, Raquel, Solano, Beatriz, Vicente, Esther, Silanes, Silvia Pérez, Aldana, Ignacio, Monge, Antonio, Sauvain, Michel, Deharo, Eric
FONTE
Memórias do Instituto Oswaldo Cruz
DATA DE PUBLICAÇÃO
2008-12
RESUMO
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 R3', R4' and R5'. (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.
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