Artemisinin-quinoline hybrid-dimers: synthesis and in vitro antiplasmodial activity

Bioorg Med Chem Lett. 2010 Dec 1;20(23):6975-7. doi: 10.1016/j.bmcl.2010.09.130. Epub 2010 Oct 21.

Abstract

Novel artemisinin-quinoline hybrid-dimers were synthesized from dihydroartemisinin and different aminoquinolines at elevated temperatures (90-110°C). All compounds were obtained as the β-isomers and were tested against both chloroquine sensitive and resistant strains of Plasmodium falciparum. Hybrid-dimer 8 showed the highest antiplasmodial activity, inheriting the optimum chain length of three carbon atoms.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antimalarials / chemical synthesis*
  • Antimalarials / chemistry
  • Artemisinins / chemistry*
  • Artemisinins / pharmacology
  • Chloroquine / pharmacology
  • Dimerization
  • Drug Resistance*
  • Plasmodium falciparum / drug effects*
  • Quinolines / chemistry*
  • Quinolines / pharmacology

Substances

  • Antimalarials
  • Artemisinins
  • Quinolines
  • Chloroquine