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
Artigo
em Inglês
| LILACS
| ID: lil-502297
Biblioteca responsável:
BR1.1
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.
Texto completo:
Disponível
Coleções:
Bases de dados internacionais
Contexto em Saúde:
Doenças Negligenciadas
Problema de saúde:
Zoonoses
Base de dados:
LILACS
Assunto principal:
Quinoxalinas
/
Leishmania mexicana
/
Óxidos N-Cíclicos
/
Antiprotozoários
Limite:
Animais
Idioma:
Inglês
Revista:
Mem. Inst. Oswaldo Cruz
Assunto da revista:
Medicina Tropical
/
Parasitologia
Ano de publicação:
2008
Tipo de documento:
Artigo
País de afiliação:
França
/
Peru
/
Espanha
Instituição/País de afiliação:
Universidad Peruana Cayetano Heredia/PE
/
University of Navarra/ES