New acyl derivatives of 3-aminofurazanes and their antiplasmodial activities

Theresa Hermann, Patrick Hochegger*, Johanna Dolensky, Werner Seebacher, Robert Saf, Marcel Kaiser, Pascal Mäser, Robert Weis

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review


An N-acylated furazan-3-amine of a Medicines for Malaria Venture (MMV) project has shown activity against different strains of Plasmodium falciparum. Seventeen new derivatives were prepared and tested in vitro for their activities against blood stages of two strains of Plasmodium falciparum. Several structure–activity relationships were revealed. The activity strongly depended on the nature of the acyl moiety. Only benzamides showed promising activity. The substitution pattern of their phenyl ring affected the activity and the cytotoxicity of compounds. In addition, physicochemical parameters were calculated (log P, log D, ligand efficiency) or determined experimentally (permeability) via a PAMPA. The N-(4-(3,4-diethoxyphenyl)-1,2,5-oxadiazol-3-yl)-3(trifluoromethyl)benzamide possessed good physicochemical properties and showed high antiplasmodial activity against a chloroquine-sensitive strain (IC50 (NF54) = 0.019 µM) and even higher antiplasmodial activity against a multiresistant strain (IC50 (K1 ) = 0.007 µM). Compared to the MMV compound, the permeability and the activity against the multiresistant strain were improved.

Original languageEnglish
Article number412
Issue number5
Publication statusPublished - May 2021


  • Antimalarial
  • Furazan derivatives
  • Plasmodium falciparum

ASJC Scopus subject areas

  • Molecular Medicine
  • Pharmaceutical Science
  • Drug Discovery


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