Synthesis and antiplasmodial activity of 3-furyl and 3-thienylquinoxaline-2-carbonitrile 1,4-di-N-oxide derivatives.
Esther
Vicente
;
Sarah
Charnaud
;
Emily
Bongard
;
Raquel
Villar
;
Asunción
Burguete
;
Beatriz
Solano
;
Saioa
Ancizu
;
Silvia
Pérez-Silanes
;
Ignacio
Aldana
;
Livia
Vivas
;
+1 more...
Antonio
Monge
;
(2008)
Synthesis and antiplasmodial activity of 3-furyl and 3-thienylquinoxaline-2-carbonitrile 1,4-di-N-oxide derivatives.
Molecules (Basel, Switzerland), 13 (1).
pp. 69-77.
ISSN 1420-3049
DOI: 10.3390/molecules13010069
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.
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