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New Amide Derivatives of Quinoxaline 1,4-di-N-Oxide with Leishmanicidal and Antiplasmodial Activities
Unidad de Investigación y Desarrollo de Nuevos Medicamentos, Centro de Investigación en Farmacobiología Aplicada (CIFA), Universidad de Navarra, Pamplona 31080, Spain
Grupo Malaria, Facultad de Medicina, Universidad de Antioquia, 050010 Medellín, Colombia
Programa de Biología, Facultad de Ciencias Básicas, Universidad del Atlántico, 080001 Barranquilla, Colombia
Université de Toulouse, UPS, UMR 152 Pharma-DEV, Université Toulouse 3, Faculté des Sciences Pharmaceutiques, F-31062 Toulouse cedex 09, France
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; in revised form: 11 April 2013 / Accepted: 18 April 2013 / Published: 22 April 2013
Abstract: 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
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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.
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(4):4718-4727.
Barea, Carlos; Pabón, Adriana; Pérez-Silanes, Silvia; Galiano, Silvia; Gonzalez, German; Monge, Antonio; Deharo, Eric; Aldana, Ignacio. 2013. "New Amide Derivatives of Quinoxaline 1,4-di-N-Oxide with Leishmanicidal and Antiplasmodial Activities." Molecules 18, no. 4: 4718-4727.