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
Keywords: 
Quinoxaline
Anti-leishmanial
Structure-activity
Leishmaniasis
Issue Date: 
2008
Publisher: 
Instituto Oswaldo Cruz, Ministério da Saúde
ISSN: 
0074-0276
Citation: 
Burguete A, Estevez Y, Castillo D, González G, Villar R, Solano B, et al. 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. Mem Inst Oswaldo Cruz. Dec 2008;103(8):778-780
Abstract
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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