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-phenylquinoxaline- 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: Vicente, E. (Esther)|||/items/f24efa36-5351-4710-a5e3-f969b2caa7fb, Charnaud, S. (Sarah)|||/items/6333ae44-3d96-45b9-abb9-46bdc4cd4395, Bongard, E. (Emily)|||/items/0f1efa2a-8066-47b5-9ab9-3cb7427aae16, Villar, R. (Raquel)|||/items/8b76d05b-786e-4baa-8e1f-5d29011d72fd, Burguete, A. (Asunción)|||/items/841509d2-131f-45ab-97cb-0e072035c61e, Solano, B. (Beatriz)|||/items/f8ed6dbf-02f6-4dec-8dcc-af6680ab51e5, Ancizu, S. (Saioa)|||/items/b7ddb356-5d8e-4be4-a223-63fbcd1a34e7, Pérez-Silanes, S. (Silvia)|||/items/e5734c65-2dd8-4fdd-a74a-fc7526136c45, Aldana, I. (Ignacio)|||/items/2a317afc-d6ab-4970-8bac-41d9715f5618, Vivas, L. (Livia)|||/items/b3009dac-3bd1-4076-bcf1-52f46642655e, Monge, A. (Antonio)|||/items/804a350e-c7ff-4318-9742-cdc3432eb2a8
Tipo de recurso: artículo
Fecha de publicación:2008
País:España
Institución:Universidad de Navarra
Repositorio:Dadun. Depósito Académico Digital de la Universidad de Navarra
Idioma:inglés
OAI Identifier:oai:dadun.unav.edu:10171/23597
Acceso en línea:https://hdl.handle.net/10171/23597
Access Level:acceso abierto
Palabra clave:Quinoxaline
N-oxides
Malaria
Antiplasmodial
P.falciparum
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-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.

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