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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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/
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spelling doaj-84eca9e233f149df82485969c6dea4b02020-11-24T22:02:29ZengMDPI AGMolecules1420-30492008-01-01131697710.3390/molecules13010069Synthesis and Antiplasmodial Activity of 3-Furyl and 3-Thienylquinoxaline-2-carbonitrile 1,4-Di-N-oxide DerivativesAntonio MongeLivia VivasIgnacio AldanaSilvia Pérez-SilanesSaioa AncizuBeatriz SolanoAsunción BurgueteRaquel VillarEmily BongardSarah CharnaudEsther VicenteThe 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.http://www.mdpi.com/1420-3049/13/1/69/QuinoxalineN-oxidesmalariaantiplasmodialP. falciparum.
collection DOAJ
language English
format Article
sources DOAJ
author Antonio Monge
Livia Vivas
Ignacio Aldana
Silvia Pérez-Silanes
Saioa Ancizu
Beatriz Solano
Asunción Burguete
Raquel Villar
Emily Bongard
Sarah Charnaud
Esther Vicente
spellingShingle Antonio Monge
Livia Vivas
Ignacio Aldana
Silvia Pérez-Silanes
Saioa Ancizu
Beatriz Solano
Asunción Burguete
Raquel Villar
Emily Bongard
Sarah Charnaud
Esther Vicente
Synthesis and Antiplasmodial Activity of 3-Furyl and 3-Thienylquinoxaline-2-carbonitrile 1,4-Di-N-oxide Derivatives
Molecules
Quinoxaline
N-oxides
malaria
antiplasmodial
P. falciparum.
author_facet Antonio Monge
Livia Vivas
Ignacio Aldana
Silvia Pérez-Silanes
Saioa Ancizu
Beatriz Solano
Asunción Burguete
Raquel Villar
Emily Bongard
Sarah Charnaud
Esther Vicente
author_sort Antonio Monge
title Synthesis and Antiplasmodial Activity of 3-Furyl and 3-Thienylquinoxaline-2-carbonitrile 1,4-Di-N-oxide Derivatives
title_short Synthesis and Antiplasmodial Activity of 3-Furyl and 3-Thienylquinoxaline-2-carbonitrile 1,4-Di-N-oxide Derivatives
title_full Synthesis and Antiplasmodial Activity of 3-Furyl and 3-Thienylquinoxaline-2-carbonitrile 1,4-Di-N-oxide Derivatives
title_fullStr Synthesis and Antiplasmodial Activity of 3-Furyl and 3-Thienylquinoxaline-2-carbonitrile 1,4-Di-N-oxide Derivatives
title_full_unstemmed Synthesis and Antiplasmodial Activity of 3-Furyl and 3-Thienylquinoxaline-2-carbonitrile 1,4-Di-N-oxide Derivatives
title_sort synthesis and antiplasmodial activity of 3-furyl and 3-thienylquinoxaline-2-carbonitrile 1,4-di-n-oxide derivatives
publisher MDPI AG
series Molecules
issn 1420-3049
publishDate 2008-01-01
description 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.
topic Quinoxaline
N-oxides
malaria
antiplasmodial
P. falciparum.
url http://www.mdpi.com/1420-3049/13/1/69/
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