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 against Plasmodium falciparum based on our previous research carried out on 3-phenyl-quinoxaline-2-carbonitrile 1,4-di-N-oxide derivatives. Twelve compounds were synthesized and evaluated for antimalarial activity. Eight of them showed an IC...

Descripción completa

Detalles Bibliográficos
Autores principales: Vicente, Esther, Charnaud, Sarah, Bongard, Emily, Villar, Raquel, Burguete, Asunción, Solano, Beatriz, Ancizu, Saioa, Pérez-Silanes, Silvia, Aldana, Ignacio, Vivas, Livia, Monge, Antonio
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2008
Materias:
Full Paper
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6245472/
https://www.ncbi.nlm.nih.gov/pubmed/18259130
http://dx.doi.org/10.3390/molecules13010069
_version_ 1783372248396070912
author Vicente, Esther
Charnaud, Sarah
Bongard, Emily
Villar, Raquel
Burguete, Asunción
Solano, Beatriz
Ancizu, Saioa
Pérez-Silanes, Silvia
Aldana, Ignacio
Vivas, Livia
Monge, Antonio
author_facet Vicente, Esther
Charnaud, Sarah
Bongard, Emily
Villar, Raquel
Burguete, Asunción
Solano, Beatriz
Ancizu, Saioa
Pérez-Silanes, Silvia
Aldana, Ignacio
Vivas, Livia
Monge, Antonio
author_sort Vicente, Esther
collection PubMed
description The aim of this study was to identify new compounds active against Plasmodium falciparum based on our previous research carried out on 3-phenyl-quinoxaline-2-carbonitrile 1,4-di-N-oxide derivatives. Twelve compounds were synthesized and evaluated for antimalarial activity. Eight of them showed an IC(50) < 1 μM against the 3D7 strain. Derivative 1 demonstrated high potency (IC(50)= 0.63 µM) and good selectivity (SI=10.35), thereby becoming a new lead-compound.
format Online
Article
Text
id pubmed-6245472
institution National Center for Biotechnology Information
language English
publishDate 2008
publisher MDPI
record_format MEDLINE/PubMed
spelling pubmed-62454722018-11-26 Synthesis and Antiplasmodial Activity of 3-Furyl and 3-Thienylquinoxaline-2-carbonitrile 1,4-Di-N-oxide Derivatives † Vicente, Esther Charnaud, Sarah Bongard, Emily Villar, Raquel Burguete, Asunción Solano, Beatriz Ancizu, Saioa Pérez-Silanes, Silvia Aldana, Ignacio Vivas, Livia Monge, Antonio Molecules Full Paper The aim of this study was to identify new compounds active against Plasmodium falciparum based on our previous research carried out on 3-phenyl-quinoxaline-2-carbonitrile 1,4-di-N-oxide derivatives. Twelve compounds were synthesized and evaluated for antimalarial activity. Eight of them showed an IC(50) < 1 μM against the 3D7 strain. Derivative 1 demonstrated high potency (IC(50)= 0.63 µM) and good selectivity (SI=10.35), thereby becoming a new lead-compound. MDPI 2008-01-17 /pmc/articles/PMC6245472/ /pubmed/18259130 http://dx.doi.org/10.3390/molecules13010069 Text en © 2008 by MDPI (http://www.mdpi.org). Reproduction is permitted for noncommercial purposes.
spellingShingle Full Paper
Vicente, Esther
Charnaud, Sarah
Bongard, Emily
Villar, Raquel
Burguete, Asunción
Solano, Beatriz
Ancizu, Saioa
Pérez-Silanes, Silvia
Aldana, Ignacio
Vivas, Livia
Monge, Antonio
Synthesis and Antiplasmodial Activity of 3-Furyl and 3-Thienylquinoxaline-2-carbonitrile 1,4-Di-N-oxide Derivatives †
title 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_short 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 †
topic Full Paper
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6245472/
https://www.ncbi.nlm.nih.gov/pubmed/18259130
http://dx.doi.org/10.3390/molecules13010069
work_keys_str_mv AT vicenteesther synthesisandantiplasmodialactivityof3furyland3thienylquinoxaline2carbonitrile14dinoxidederivatives
AT charnaudsarah synthesisandantiplasmodialactivityof3furyland3thienylquinoxaline2carbonitrile14dinoxidederivatives
AT bongardemily synthesisandantiplasmodialactivityof3furyland3thienylquinoxaline2carbonitrile14dinoxidederivatives
AT villarraquel synthesisandantiplasmodialactivityof3furyland3thienylquinoxaline2carbonitrile14dinoxidederivatives
AT burgueteasuncion synthesisandantiplasmodialactivityof3furyland3thienylquinoxaline2carbonitrile14dinoxidederivatives
AT solanobeatriz synthesisandantiplasmodialactivityof3furyland3thienylquinoxaline2carbonitrile14dinoxidederivatives
AT ancizusaioa synthesisandantiplasmodialactivityof3furyland3thienylquinoxaline2carbonitrile14dinoxidederivatives
AT perezsilanessilvia synthesisandantiplasmodialactivityof3furyland3thienylquinoxaline2carbonitrile14dinoxidederivatives
AT aldanaignacio synthesisandantiplasmodialactivityof3furyland3thienylquinoxaline2carbonitrile14dinoxidederivatives
AT vivaslivia synthesisandantiplasmodialactivityof3furyland3thienylquinoxaline2carbonitrile14dinoxidederivatives
AT mongeantonio synthesisandantiplasmodialactivityof3furyland3thienylquinoxaline2carbonitrile14dinoxidederivatives

Ejemplares similares