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

Patrick Hochegger, Johanna Faist, Werner Seebacher, Robert Saf, Pascal Maeser, Marcel Kaiser, Robert Weis*

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

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.
Original languageEnglish
Pages (from-to)2251-2259
JournalBioorganic & Medicinal Chemistry
Volume25
Issue number7
DOIs
Publication statusPublished - 2017

Treatment code (Nähere Zuordnung)

  • Basic - Fundamental (Grundlagenforschung)

Fingerprint

Dive into the research topics of 'New derivatives of quinoline-4-carboxylic acid with antiplasmodial activity'. Together they form a unique fingerprint.
  • Mass Spectrometry

    Saf, R. & Bartl, K.

    1/01/95 → …

    Project: Research area

Cite this