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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