Synthesis and antiplasmodial activity of 3-furyl and 3-thienylquinoxaline-2-carbonitrile 1,4-di-N-oxide derivatives

Vicente, E. (Esther); Charnaud, S. (Sarah); Bongard, E. (Emily); Raquel; Burguete, A. (Asunción); Solano, B. (Beatriz); Ancizu, S. (Saioa); Pérez-Silanes, S. (Silvia); Aldana, I. (Ignacio); Vivas, L. (Livia); Monge, A. (Antonio)

Palabras clave :

Quinoxaline
N-oxides
Malaria
Antiplasmodial
P.falciparum

Fecha de publicación :

2008

Editorial :

MDPI

Versión del Editor:

http://www.mdpi.com/journal/molecules

ISSN :

1420-3049

Cita:

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.

Resumen

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.

URI :

https://hdl.handle.net/10171/23597

Aparece en las colecciones:

DA - CIFA - I+D de medicamentos - Artículos de revistas
DA - Farmacia - Orgánica - Artículos de revista

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