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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
, 1
, 1,4
, 1
, 5
, 1
 and 1
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 which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.

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MDPI and ACS Style

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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