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Synthesis and antiplasmodial activity of 3-furyl and 3-thienylquinoxaline-2-carbonitrile 1,4-di-N-oxide derivatives
Authors: Vicente, E. (Esther)
Charnaud, S. (Sarah)
Bongard, E. (Emily)
Villar, R. (Raquel)
Burguete, A. (Asunción)
Solano, B. (Beatriz)
Ancizu, S. (Saioa)
Perez-Silanes, S. (Silvia)
Aldana, I. (Ignacio)
Vivas, L. (Livia)
Monge, A. (Antonio)
Keywords: Quinoxaline
N-oxides
Malaria
Antiplasmodial
P.falciparum
Issue Date: 2008
Publisher: MDPI
Publisher version: http://www.mdpi.com/journal/molecules
ISSN: 1420-3049
Citation: Vicente E, Charnaud S, Bongard E, Villar R, Burguete A, Solano B, et al. Synthesis and antiplasmodial activity of 3-furyl and 3-thienylquinoxaline-2-carbonitrile 1,4-di-N-oxide derivatives. Molecules 2008 Jan 17;13(1):69-77.
Abstract
The aim of this study was to identify new compounds active against Plasmodium falciparum based on our previous research carried out on 3-phenylquinoxaline- 2-carbonitrile 1,4-di-N-oxide derivatives. Twelve compounds were synthesized and evaluated for antimalarial activity. Eight of them showed an IC50 < 1 μM against the 3D7 strain. Derivative 1 demonstrated high potency (IC50= 0.63 μM) and good selectivity (SI=10.35), thereby becoming a new lead-compound.
Permanent link: http://hdl.handle.net/10171/23597
Appears in Collections:DA - Farmacia - Orgánica - Artículos de revista
DA - CIFA - I+D de medicamentos - Artículos de revistas

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