Synthesis of ring-substituted 4-aminoquinolines and evaluation of their antimalarial activities

Bioorg Med Chem Lett. 2005 Feb 15;15(4):1015-8. doi: 10.1016/j.bmcl.2004.12.037.


A simple two-step synthesis method was used to make 51 B-ring-substituted 4-hydroxyquinolines allowing analysis of the effect of ring substitutions on inhibition of growth of chloroquine sensitive and resistant strains of Plasmodium falciparum, the dominant cause of malaria morbidity. Substituted quinoline rings other than the 7-chloroquinoline ring found in chloroquine were found to have significant activity against the drug-resistant strain of P. falciparum W2.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Aminoquinolines / chemical synthesis*
  • Aminoquinolines / pharmacology
  • Animals
  • Antimalarials / chemical synthesis*
  • Antimalarials / pharmacology
  • Chloroquine / pharmacology
  • Drug Resistance
  • Plasmodium falciparum / drug effects
  • Structure-Activity Relationship


  • Aminoquinolines
  • Antimalarials
  • Chloroquine
  • 4-aminoquinoline