Quinolines and structurally related heterocycles as antimalarials

Eur J Med Chem. 2010 Aug;45(8):3245-64. doi: 10.1016/j.ejmech.2010.04.011. Epub 2010 Apr 18.


The quinoline scaffold is prevalent in a variety of pharmacologically active synthetic and natural compounds. The discovery of chloroquine, the most famous drug containing this scaffold resulted in control and eradication of malaria for decades. The other known antimalarial drugs from the quinoline family include: quinine, amodiaquine, piperaquine, primaquine, and mefloquine. The drugs from this group mostly act during the blood stages of the parasite's life cycle but some like primaquine targets the tissue stages. This review provides a comprehensive literature compilation concerning the study of quinolines and also other heterocycles structurally similar to quinoline scaffold in the treatment of malaria. This review covers advances made in the last ten years and it is subdivided into eight sub-headings. It consists of discussion on the biological activities, structure-activity relationship, and potential biochemical pathways of 4-aminoquinolines, 4-anilinoquinolines, 8-aminoquinolines, quinolines from nature, quinolones, isoquinolines and tetrahydroquinolines, ring-modified quinolines, and miscellaneous quinolines.

Publication types

  • Review

MeSH terms

  • Animals
  • Antimalarials / chemistry*
  • Antimalarials / pharmacology*
  • Humans
  • Quinolines / chemistry*
  • Quinolines / pharmacology*
  • Structure-Activity Relationship


  • Antimalarials
  • Quinolines