Burguete A., Estevez Y., Castillo D., Gonzalez G., Villar R., Solano B., Vicente E., Silanes S. P., Aldana I., Monge A., Sauvain Michel, Deharo Eric. (2008). 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. Memorias do Instituto Oswaldo Cruz, 103 (8), p. 778-780. ISSN 0074-0276.
Titre du document
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
Année de publication
2008
Auteurs
Burguete A., Estevez Y., Castillo D., Gonzalez G., Villar R., Solano B., Vicente E., Silanes S. P., Aldana I., Monge A., Sauvain Michel, Deharo Eric
Source
Memorias do Instituto Oswaldo Cruz, 2008,
103 (8), p. 778-780 ISSN 0074-0276
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 R-3', R-4' and R-5'. (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.
Plan de classement
Entomologie médicale / Parasitologie / Virologie [052]
Localisation
Fonds IRD [F B010044228]
Identifiant IRD
fdi:010044228
