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Molecules 2008, 13(1), 69-77; doi:10.3390/molecules13010069

Synthesis and Antiplasmodial Activity of 3-Furyl and 3-Thienylquinoxaline-2-carbonitrile 1,4-Di-N-oxide Derivatives

Unidad de Investigación y Desarrollo de Medicamentos, Centro de Investigación en Farmacobiología Aplicada (CIFA), University of Navarra, 31080 Pamplona, Spain
Department of Infectious and Tropical Diseases, London School of Hygiene and Tropical Medicine (LSHTM), Keppel Street, London WC1E 7HT, UK
Author to whom correspondence should be addressed.
Received: 18 December 2007 / Accepted: 11 January 2008 / Published: 17 January 2008
(This article belongs to the Special Issue ECSOC-11)
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The aim of this study was to identify new compounds active againstPlasmodium falciparum based on our previous research carried out on 3-phenylquinoxaline-2-carbonitrile 1,4-di-N-oxide derivatives. Twelve compounds weresynthesized and evaluated for antimalarial activity. Eight of them showed an IC50 less than 1 μMagainst the 3D7 strain. Derivative 1 demonstrated high potency (IC50= 0.63 μM) and goodselectivity (SI=10.35), thereby becoming a new lead-compound. View Full-Text
Keywords: Quinoxaline; N-oxides; malaria; antiplasmodial; P. falciparum. Quinoxaline; N-oxides; malaria; antiplasmodial; P. falciparum.

Figure 1

This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Vicente, E.; Charnaud, S.; Bongard, E.; Villar, R.; Burguete, A.; Solano, B.; Ancizu, S.; Pérez-Silanes, S.; Aldana, I.; Vivas, L.; Monge, A. Synthesis and Antiplasmodial Activity of 3-Furyl and 3-Thienylquinoxaline-2-carbonitrile 1,4-Di-N-oxide Derivatives. Molecules 2008, 13, 69-77.

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