Synthesis and antiplasmodial activity of 3-furyl and 3-thienylquinoxaline-2-carbonitrile 1,4-di-N-oxide derivatives.

EstherVicente; SarahCharnaud; EmilyBongard; RaquelVillar; AsunciónBurguete; BeatrizSolano; SaioaAncizu; SilviaPérez-Silanes; IgnacioAldana; LiviaVivas; +1 more... AntonioMonge; (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

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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.

Item Type	Article
ISI	252812700007

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