New amide derivatives of quinoxaline 1,4-di-N-oxide with leishmanicidal and antiplasmodial activities

ABSTARCT: Malaria and leishmaniasis are two of the World’s most important tropical parasitic diseases. Continuing with our efforts to identify new compounds active against malaria and leishmaniasis, twelve new 1,4-di-N-oxide quinoxaline derivatives were synthesized and evaluated for their in vitro a...

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Detalles Bibliográficos
Autores: Barea, Carlos, Pabón Vidal, Adriana Lucía, Pérez Silanes, Silvia, Galiano, Silvia, González, Germán, Monge, Antonio, Deharo, Eric, Aldana Moraza, Ignacio
Tipo de recurso: artículo
Estado:Versión publicada
Fecha de publicación:2013
País:Colombia
Institución:Universidad de Antioquia
Repositorio:Repositorio UdeA
Idioma:inglés
OAI Identifier:oai:bibliotecadigital.udea.edu.co:10495/7889
Acceso en línea:http://hdl.handle.net/10495/7889
Access Level:acceso abierto
Palabra clave:Antiplasmodial
Leishmanicidal
Quinoxaline
Descripción
Sumario:ABSTARCT: Malaria and leishmaniasis are two of the World’s most important tropical parasitic diseases. Continuing with our efforts to identify new compounds active against malaria and leishmaniasis, twelve new 1,4-di-N-oxide quinoxaline derivatives were synthesized and evaluated for their in vitro antimalarial and antileishmanial activity against Plasmodium falciparum FCR-3 strain, Leishmania infantum and Leishmania amazonensis. Their toxicity against VERO cells (normal monkey kidney cells) was also assessed. The results obtained indicate that a cyclopentyl derivative had the best antiplasmodial activity (2.9 µM), while a cyclohexyl derivative (2.5 µM) showed the best activity against L. amazonensis, and a 3-chloropropyl derivative (0.7 µM) showed the best results against L. infantum. All these compounds also have a Cl substituent in the R7 position