Molecules (Jan 2008)

Synthesis and Antiplasmodial Activity of 3-Furyl and 3-Thienylquinoxaline-2-carbonitrile 1,4-Di-N-oxide Derivatives

  • Antonio Monge,
  • Livia Vivas,
  • Ignacio Aldana,
  • Silvia Pérez-Silanes,
  • Saioa Ancizu,
  • Beatriz Solano,
  • Asunción Burguete,
  • Raquel Villar,
  • Emily Bongard,
  • Sarah Charnaud,
  • Esther Vicente

DOI
https://doi.org/10.3390/molecules13010069
Journal volume & issue
Vol. 13, no. 1
pp. 69 – 77

Abstract

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The aim of this study was to identify new compounds active againstPlasmodium falciparum based on our previous research carried out on 3-phenylquinoxaline-2-carbonitrile 1,4-di-N-oxide derivatives. Twelve compounds weresynthesized and evaluated for antimalarial activity. Eight of them showed an IC50 less than 1 μMagainst the 3D7 strain. Derivative 1 demonstrated high potency (IC50= 0.63 μM) and goodselectivity (SI=10.35), thereby becoming a new lead-compound.

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