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

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 antimalaria...

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Autores: Barea, C. (Carlos)|||/items/4f4c9d7c-4235-491b-9444-7a90d51c223d, Pabon, A. (Adriana)|||/items/49b4dd33-b935-4fa8-bfc7-8bb9e2a92b49, Pérez-Silanes, S. (Silvia)|||/items/e5734c65-2dd8-4fdd-a74a-fc7526136c45, Galiano, S. (Silvia)|||/items/10b9d373-6e6e-46e4-bfae-e7b241dad5fd, Gonzalez, G. (Germán)|||/items/c2dc077d-6791-48a8-ae3e-3b6e5bded95b, Monge, A. (Antonio)|||/items/804a350e-c7ff-4318-9742-cdc3432eb2a8, Deharo, E. (Eric)|||/items/48bf3a09-fa0f-4898-8f39-dce9f0fcdef9, Aldana, I. (Ignacio)|||/items/2a317afc-d6ab-4970-8bac-41d9715f5618
Tipo de recurso: artículo
Fecha de publicación:2013
País:España
Institución:Universidad de Navarra
Repositorio:Dadun. Depósito Académico Digital de la Universidad de Navarra
Idioma:inglés
OAI Identifier:oai:dadun.unav.edu:10171/29506
Acceso en línea:https://hdl.handle.net/10171/29506
Access Level:acceso abierto
Palabra clave:Quinoxaline
1,4-di-N-oxide
Leishmanicidal
Antiplasmodial
Descripción
Sumario: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.