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., Monge A.
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. © 2008 by MDPI.