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

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

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...

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Bibliographic Details
Main Authors: Antonio Monge, Livia Vivas, Ignacio Aldana, Silvia Pérez-Silanes, Saioa Ancizu, Beatriz Solano, Asunción Burguete, Raquel Villar, Emily Bongard, Sarah Charnaud, Esther Vicente
Format: Article
Language:English
Published: MDPI AG 2008-01-01
Series:Molecules
Subjects:
Quinoxaline
N-oxides
malaria
antiplasmodial
P. falciparum.
Online Access:http://www.mdpi.com/1420-3049/13/1/69/
Description
Summary: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.
ISSN:1420-3049

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