Synthesis of 2,4-disubstituted 6-methoxy-8-aminoquinoline analogues as potential antiparasitics

J Med Chem. 1980 May;23(5):581-4. doi: 10.1021/jm00179a023.

Abstract

A series of 2,4-disubstituted 8-aminoquinoline analogues were synthesized and evaluated against Plasmodium berghei in mice and Leishmania donovani in hamsters. 8-[[6-(Diethylamino)hexyl]amino]-2-ethyl-6-methoxy-4-methylquinoline (8a) possessed significant activity against L. donovani. 2-Ethyl-4-methylprimaquine (7a) was evaluated against Plasmodium cynomolgi in rhesus monkey and found to have activity equal to that of primaquine.

Publication types

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

MeSH terms

  • Aminoquinolines / chemical synthesis*
  • Aminoquinolines / pharmacology
  • Animals
  • Antimalarials / chemical synthesis
  • Antiprotozoal Agents / chemical synthesis*
  • Chemical Phenomena
  • Chemistry
  • Haplorhini
  • Leishmania / drug effects
  • Macaca mulatta
  • Malaria / drug therapy
  • Plasmodium / drug effects

Substances

  • Aminoquinolines
  • Antimalarials
  • Antiprotozoal Agents