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• Barea, C
• Pabón, A
• Galiano, S
• Pérez-Silanes, S
• Gonzalez, G
• Deyssard, C
• Monge, A
• Deharo, E
• Aldana, I
• [+] on Google Scholar
• Barea, C
• Pabón, A
• Galiano, S
• Pérez-Silanes, S
• Gonzalez, G
• Deyssard, C
• Monge, A
• Deharo, E
• Aldana, I
• [+] on PubMed
• Barea, C
• Pabón, A
• Galiano, S
• Pérez-Silanes, S
• Gonzalez, G
• Deyssard, C
• Monge, A
• Deharo, E
• Aldana, I

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Molecules 2012, 17(8), 9451-9461; doi:10.3390/molecules17089451

Article

Antiplasmodial and Leishmanicidal Activities of 2-Cyano-3-(4-phenylpiperazine-1-carboxamido) Quinoxaline 1,4-Dioxide Derivatives

Carlos Barea ^1,* , Adriana Pabón ² , Silvia Galiano ¹ , Silvia Pérez-Silanes ¹ , German Gonzalez ^3,4 , Chloe Deyssard ^3,4 , Antonio Monge ¹ , Eric Deharo ^3,4  and Ignacio Aldana ¹

¹ Research and Development of Novel Drugs Unit, Center for Applied Pharmacobiology Research (CIFA), University of Navarre, Pamplona 31080, Spain ² Malaria Group, University of Antioquia, Medellín, Colombia ³ UMR 152 PharmaDev (Pharmacologie et Pharmacochimie pour le Développement), Université de Toulouse, UPS, 118, rte de Narbonne, F-31062 Toulouse cedex 9, France ⁴ UMR 152 PharmaDev Institut de Recherche pour le Développement, Faculté des Sciences Pharmaceutiques, Université de Toulouse 3, 31062 Toulouse, France

* Author to whom correspondence should be addressed.

Received: 28 June 2012; in revised form: 20 July 2012 / Accepted: 31 July 2012 / Published: 7 August 2012

(This article belongs to the Section Medicinal Chemistry)

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Abstract: Malaria and leishmaniasis are two of the World’s most important tropical parasitic diseases. Thirteen new 2-cyano-3-(4-phenylpiperazine-1-carboxamido) quinoxaline 1,4-dioxide derivatives (CPCQs) were synthesized and evaluated for their in vitro antimalarial and antileishmanial activity against erythrocytic forms of Plasmodium falciparum and axenic forms of Leishmania infantum. Their toxicity against VERO cells (normal monkey kidney cells) was also assessed. None of the tested compounds was efficient against Plasmodium, but two of them showed good activity against Leishmania. Toxicity on VERO was correlated with leishmanicidal properties.

Keywords: quinoxaline; piperazine; Plasmodium; Leishmania; VERO

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