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
;
103(8): 778-780, Dec. 2008. tab
Article
Dans Anglais
| LILACS
| ID: lil-502297
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.
Texte intégral:
Disponible
Indice:
LILAS (Amériques)
Sujet Principal:
Quinoxalines
/
Leishmania mexicana
/
N-oxydes cycliques
/
Antiprotozoaires
Limites du sujet:
Animaux
langue:
Anglais
Texte intégral:
Mem. Inst. Oswaldo Cruz
Thème du journal:
Médecine tropicale
/
Parasitologie
Année:
2008
Type:
Article
Pays d'affiliation:
France
/
Pérou
/
Espagne
Institution/Pays d'affiliation:
Universidad Peruana Cayetano Heredia/PE
/
University of Navarra/ES
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