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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Published in:Molecules (Basel, Switzerland) Switzerland), 2008-01, Vol.13 (1), p.69-77
Main Authors: Vicente, Esther, Charnaud, Sarah, Bongard, Emily, Villar, Raquel, Burguete, Asunción, Solano, Beatriz, Ancizu, Saioa, Pérez-Silanes, Silvia, Aldana, Ignacio, Vivas, Livia, Monge, Antonio
Format: Article
Language:English
Subjects:
Animals
Antimalarials - chemical synthesis
Antimalarials - chemistry
Antimalarials - pharmacology
Antiparasitic agents
antiplasmodial
Cell Death - drug effects
Cell Line
Cyclic N-Oxides - chemical synthesis
Cyclic N-Oxides - chemistry
Cyclic N-Oxides - pharmacology
Cytotoxicity
Drug Resistance - drug effects
Malaria
N-oxides
Nitriles - chemical synthesis
Nitriles - chemistry
Nitriles - pharmacology
Oxides - chemical synthesis
Oxides - chemistry
Oxides - pharmacology
P. falciparum
Parasitic Sensitivity Tests
Plasmodium falciparum - drug effects
Quinoxaline
Quinoxalines - chemical synthesis
Quinoxalines - chemistry
Quinoxalines - pharmacology
Tropical diseases
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Summary: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) less than 1 microM against the 3D7 strain. Derivative 1 demonstrated high potency (IC(50)= 0.63 microM) and good selectivity (SI=10.35), thereby becoming a new lead-compound.
ISSN:1420-3049
1420-3049
DOI:10.3390/molecules13010069