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
2008; Instituto Oswaldo Cruz, Ministério da Saúde; Volume: 103; Issue: 8 Linguagem: Inglês
10.1590/s0074-02762008000800006
ISSN1678-8060
AutoresAsunción Burguete, Yannick Estevez, Denis Castillo, Germán González, Raquel Villar, Beatriz Solano, Esther Vicente, Silvia Pérez‐Silanes, Ignacio Aldana, Antonio Monge, Michel Sauvain, Eric Deharo,
Tópico(s)Insect and Pesticide Research
ResumoA 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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