Reversed chloroquine molecules as a strategy to overcome resistance in malaria

Curr Top Med Chem. 2012;12(5):400-7. doi: 10.2174/156802612799362968.


This short review tells the story of how Reversed Chloroquine drugs (RCQs) were developed. These are hybrid molecules, made by combining the quinoline nucleus from chloroquine (CQ) with moieties which are designed to inhibit efflux via known transporters in the membrane of the digestive vacuole of the malaria parasite. The resulting RCQ drugs can have potencies exceeding that of CQ, while at the same time having physical chemical characteristics that may make them favorable as partner drugs in combination therapies. The need for such novel antimalarial drugs will continue for the foreseeable future.

Publication types

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

MeSH terms

  • Animals
  • Antimalarials / pharmacology
  • Antimalarials / therapeutic use
  • Chloroquine / chemistry
  • Chloroquine / pharmacology*
  • Chloroquine / therapeutic use
  • Drug Resistance / drug effects*
  • Humans
  • Malaria / drug therapy*
  • Membrane Transport Proteins / drug effects
  • Plasmodium falciparum / drug effects


  • Antimalarials
  • Membrane Transport Proteins
  • Chloroquine