4.6 Article Proceedings Paper

Synthesis and antiplasmodial activity of 3-furyl and 3-thienylquinoxaline-2-carbonitrile 1,4-Di-N-oxide Derivatives

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MOLECULES
卷 13, 期 1, 页码 69-77

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MOLECULAR DIVERSITY PRESERVATION INT
DOI: 10.3390/molecules13010069

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quinoxaline; N-oxides; malaria; antiplasmodial; P. falciparum

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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-phenylquinoxaline2- carbonitrile 1,4-di-N-oxide derivatives. Twelve compounds were synthesized and evaluated for antimalarial activity. Eight of them showed an IC50 < 1 mu M against the 3D7 strain. Derivative 1 demonstrated high potency (IC50= 0.63 mu M) and good selectivity (SI= 10.35), thereby becoming a new lead-compound.

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