8-Aminoquinolines with an Aminoxyalkyl Side Chain Exert in vitro Dual-Stage Antiplasmodial Activity

ChemMedChem. 2019 Feb 19;14(4):501-511. doi: 10.1002/cmdc.201800691. Epub 2019 Jan 14.

Abstract

A series of novel 8-aminoquinolines (8-AQs) with an aminoxyalkyl side chain were synthesized and evaluated for in vitro antiplasmodial properties against asexual blood stages, liver stages, and sexual stages of Plasmodium falciparum. 8-AQs bearing 2-alkoxy and 5-phenoxy substituents on the quinoline ring system were found to be the most promising compounds under study, exhibiting potent blood schizontocidal and moderate tissue schizontocidal in vitro activity.

Keywords: 8-aminoquinolines; antimalarials; dual-stage antiplasmodial activity; malaria.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Aminoquinolines / chemical synthesis
  • Aminoquinolines / chemistry*
  • Aminoquinolines / pharmacology
  • Antimalarials / chemical synthesis
  • Antimalarials / chemistry*
  • Antimalarials / pharmacology
  • Cell Survival / drug effects
  • Hep G2 Cells
  • Humans
  • Life Cycle Stages / drug effects
  • Plasmodium falciparum / drug effects
  • Plasmodium falciparum / growth & development*
  • Structure-Activity Relationship

Substances

  • Aminoquinolines
  • Antimalarials
  • 8-aminoquinoline