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
Data(s) |
01/12/2008
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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. |
Formato |
text/html |
Identificador |
http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0074-02762008000800006 |
Idioma(s) |
en |
Publicador |
Instituto Oswaldo Cruz, Ministério da Saúde |
Fonte |
Memórias do Instituto Oswaldo Cruz v.103 n.8 2008 |
Palavras-Chave | #quinoxaline #anti-leishmanial #structure-activity #Leishmaniasis |
Tipo |
journal article |