8-amino-6-methoxyquinoline—tetrazole hybrids: Impact of linkers on antiplasmodial activity

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

Abstract

A new series of compounds was prepared from 6-methoxyquinolin-8-amine or its N-(2-aminoethyl) analogue via Ugi-azide reaction. Their linkers between the quinoline and the tert-butyltetrazole moieties differ in chain length, basicity and substitution. Compounds were tested for their antiplasmodial activity against Plasmodium falciparum NF54 as well as their cytotoxicity against L-6-cells. The activity and the cytotoxicity were strongly influenced by the linker and its substitution. The most active compounds showed good activity and promising selectivity.

Original languageEnglish
Article number5530
JournalMolecules
Volume26
Issue number18
DOIs
Publication statusPublished - Sep 2021

Keywords

  • 8-aminoquinolines
  • Antimalarial
  • Plasmodium falciparum
  • Tetrazole derivatives

ASJC Scopus subject areas

  • Analytical Chemistry
  • Chemistry (miscellaneous)
  • Molecular Medicine
  • Pharmaceutical Science
  • Drug Discovery
  • Physical and Theoretical Chemistry
  • Organic Chemistry

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