New derivatives of quinoline-4-carboxylic acid with antiplasmodial activity

Bioorg Med Chem. 2017 Apr 1;25(7):2251-2259. doi: 10.1016/j.bmc.2017.02.043. Epub 2017 Feb 24.

Abstract

New analogues of the recently published compound DDD107498 were prepared. Their activities were examined in vitro against the chloroquine-sensitive NF54 strain. The most active were also tested against the multiresistant K1 strain of Plasmodium falciparum. A couple of the newly synthesized compounds showed promising antiplasmodial activity and selectivity. A single compound showed adequate reduction of parasitaemia (98.1%) in mice infected with Plasmodium berghei. Survival time was doubled compared to control. The results of the biological tests of the novel compounds were compared with the activities of drugs in use. Structure-activity relationships were discussed.

Keywords: Amides; Amines; Plasmodium falciparum; Quinolines.

MeSH terms

  • Animals
  • Antimalarials / chemistry
  • Antimalarials / pharmacology*
  • Parasitic Sensitivity Tests
  • Plasmodium falciparum / drug effects*
  • Quinolines / chemistry
  • Quinolines / pharmacology*
  • Spectrum Analysis / methods
  • Structure-Activity Relationship

Substances

  • Antimalarials
  • Quinolines
  • quinoline-4-carboxylic acid