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Molecules 2013, 18(4), 4718-4727; doi:10.3390/molecules18044718

New Amide Derivatives of Quinoxaline 1,4-di-N-Oxide with Leishmanicidal and Antiplasmodial Activities

1,* , 2,3, 1, 1, 4,5, 1, 4,5 and 1
1 Unidad de Investigación y Desarrollo de Nuevos Medicamentos, Centro de Investigación en Farmacobiología Aplicada (CIFA), Universidad de Navarra, Pamplona 31080, Spain 2 Grupo Malaria, Facultad de Medicina, Universidad de Antioquia, 050010 Medellín, Colombia 3 Programa de Biología, Facultad de Ciencias Básicas, Universidad del Atlántico, 080001 Barranquilla, Colombia 4 Université de Toulouse, UPS, UMR 152 Pharma-DEV, Université Toulouse 3, Faculté des Sciences Pharmaceutiques, F-31062 Toulouse cedex 09, France 5 Institut de Recherche pour le Développement (IRD), UMR 152 Pharma-DEV, F-31062 Toulouse cedex 09, France
* Author to whom correspondence should be addressed.
Received: 26 March 2013 / Revised: 11 April 2013 / Accepted: 18 April 2013 / Published: 22 April 2013
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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.
Keywords: quinoxaline; 1,4-di-N-oxide; leishmanicidal; antiplasmodial quinoxaline; 1,4-di-N-oxide; leishmanicidal; antiplasmodial
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Barea, C.; Pabón, A.; Pérez-Silanes, S.; Galiano, S.; Gonzalez, G.; Monge, A.; Deharo, E.; Aldana, I. New Amide Derivatives of Quinoxaline 1,4-di-N-Oxide with Leishmanicidal and Antiplasmodial Activities. Molecules 2013, 18, 4718-4727.

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