2. Academic Validation
  3. New derivatives of 7-chloroquinolin-4-amine with antiprotozoal activity

New derivatives of 7-chloroquinolin-4-amine with antiprotozoal activity

  • Bioorg Med Chem. 2017 Feb 1;25(3):941-948. doi: 10.1016/j.bmc.2016.12.006.
Johanna Faist 1,  Clemens Hinteregger 2,  Werner Seebacher 2,  Robert Saf 3,  Pascal Mäser 4,  Marcel Kaiser 4,  Robert Weis 2
Affiliations

Affiliations

  • 1 Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, University of Graz, Austria. Electronic address: johanna.faist@uni-graz.at.
  • 2 Institute of Pharmaceutical Sciences, Pharmaceutical Chemistry, University of Graz, Austria.
  • 3 Institute for Chemistry and Technology of Materials (ICTM), University of Technology Graz, Austria.
  • 4 Swiss Tropical and Public Health Institute, and University of Basel, Switzerland.
PMID: 28031151 DOI: 10.1016/j.bmc.2016.12.006
Abstract

Novel ω-aminoacyl and -alkyl derivatives of 7-chloroquinolin-4-amine were prepared and their structures confirmed by NMR spectroscopy. Their antiprotozoal activities were examined in vitro against the sensitive NF54 strain as well as against the multiresistant K1 strain of Plasmodium falciparum and against Trypanosoma brucei rhodesiense (STIB 900). The results were compared with the activities of clinically used drugs. Their antitrypanosomal activities were only moderate whereas their antiplasmodial activities looked very promising. Some were equal or slightly more active than chloroquine against the sensitive strain. However, in comparison to chloroquine, the activity of the new compounds was decreased much less in the resistant strain. Several possessed activity against both strains in low nanomolar concentration.

Keywords

Amines; Antiplasmodial activity; Heterocycles; NMR spectroscopy; Nucleophilic substitutions; Quinoline.

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