Synthesis and antiplasmodial activity of 3-furyl and 3-thienylquinoxaline-2-carbonitrile 1,4-di-N-oxide derivatives.
Vicente, E; Charnaud, S; Bongard, E; Villar, R; Burguete, A; Solano, B; Ancizu, S; Pérez-Silanes, S; Aldana, I; Vivas, L; +1 more...Monge, A and
(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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