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

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

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  • Journal Molecules (Basel, Switzerland)

  • Published 17 Jan 2008

  • Volume 13

  • ISSUE 1

  • Pagination 69-77

  • DOI 10.3390/molecules13010069

Abstract

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.