2. Academic Validation
  3. New derivatives of quinoline-4-carboxylic acid with antiplasmodial activity

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.
Patrick Hochegger 1,  Johanna Faist 1,  Werner Seebacher 1,  Robert Saf 2,  Pascal Mäser 3,  Marcel Kaiser 3,  Robert Weis 4
Affiliations

Affiliations

  • 1 Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, University of Graz, Schubertstraße 1, A-8010 Graz, Austria.
  • 2 Institute for Chemistry and Technology of Materials (ICTM), University of Technology, Stremayrgasse 9, A-8010 Graz, Austria.
  • 3 Swiss Tropical and Public Health Institute, Socinstrasse 57, Basel CH-4002, Switzerland; University of Basel, Petersplatz 1, Basel 4003, Switzerland.
  • 4 Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, University of Graz, Schubertstraße 1, A-8010 Graz, Austria. Electronic address: robert.weis@uni-graz.at.
PMID: 28279559 DOI: 10.1016/j.bmc.2017.02.043
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.

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