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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Detalhes bibliográficos
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 documento: artigo
Data de publicação:2013
País:España
Recursos:Universidad de Navarra
Repositório:Dadun. Depósito Académico Digital de la Universidad de Navarra
Idioma:inglês
OAI Identifier:oai:dadun.unav.edu:10171/29506
Acesso em linha:https://hdl.handle.net/10171/29506
Access Level:Acceso aberto
Palavra-chave:Quinoxaline
1,4-di-N-oxide
Leishmanicidal
Antiplasmodial
Descrição
Resumo: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.