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Molecules 2014, 19(2), 2166-2180; doi:10.3390/molecules19022166
Article

Synthesis, Biological Evaluation and Structure-Activity Relationships of New Quinoxaline Derivatives as Anti-Plasmodium falciparum Agents

1,* , 2,3
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1 Unidad de Investigación y Desarrollo de Medicamentos, Centro de Investigación en Farmacobiología Aplicada (CIFA), Universidad de Navarra, c/ Irunlarrea 1, Pamplona 31008, Spain 2 Grupo Malaria, Facultad de Medicina, Universidad de Antioquia, Medellín 050010, Colombia 3 Programa de Biología, Facultad de Ciencias Básicas, Universidad del Atlántico, Barranquilla 080001, Colombia 4 Instituto de Química Avanzada de Cataluña, Consejo Superior de Investigaciones Científicas (CSIC), c/ Jordi Girona 18-26, Barcelona 08034, Spain 5 PHARMA-DEV, UMR 152 IRD-UPS, Faculté des Sciences Pharmaceutiques, Université Paul Sabatier, 35 chemin des Maraîchers, 31062 Toulouse Cedex 09, France
* Author to whom correspondence should be addressed.
Received: 10 January 2014 / Revised: 8 February 2014 / Accepted: 10 February 2014 / Published: 18 February 2014
(This article belongs to the Section Medicinal Chemistry)
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Abstract

We report the synthesis and antimalarial activities of eighteen quinoxaline and quinoxaline 1,4-di-N-oxide derivatives, eight of which are completely novel. Compounds 1a and 2a were the most active against Plasmodium falciparum strains. Structure-activity relationships demonstrated the importance of an enone moiety linked to the quinoxaline ring.
Keywords: Plasmodium falciparum; antimalarial agents; quinoxaline; quinoxaline 1,4-di-N-oxide; chalcone Plasmodium falciparum; antimalarial agents; quinoxaline; quinoxaline 1,4-di-N-oxide; chalcone
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Gil, A.; Pabón, A.; Galiano, S.; Burguete, A.; Pérez-Silanes, S.; Deharo, E.; Monge, A.; Aldana, I. Synthesis, Biological Evaluation and Structure-Activity Relationships of New Quinoxaline Derivatives as Anti-Plasmodium falciparum Agents. Molecules 2014, 19, 2166-2180.

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