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


Autoria(s): 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
Data(s)

01/12/2008

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