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...

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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
Descripción
Sumario: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.

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