In vivo and in vitro antimalarial effect and toxicological evaluation of the chloroquine analogue PQUI08001/06

Parasitol Res. 2018 Nov;117(11):3585-3590. doi: 10.1007/s00436-018-6057-6. Epub 2018 Aug 25.

Abstract

Antimalarial interventions mostly rely upon drugs, as chloroquine. However, plasmodial strains resistant to many drugs are constantly reported, leading to an expansion of malaria cases. Novel approaches are required to circumvent the drug resistance issue. Here, we describe the antimalarial potential of the chloroquine analogue 2-[[2-[(7-chloro-4-quinolinyl)amino]ethyl]amino] ethanol (PQUI08001/06). We observed that PQUI08001/06 treatment reduces parasitemia of both chloroquine-resistant and -sensitive strains of Plasmodium falciparum in vitro and P. berghei in vivo. Our data suggests that PQUI08001/06 is a potential antimalarial therapeutic alternative approach that could also target chloroquine-resistant plasmodial strains.

Keywords: Antimalarial drug; Chloroquine; Chloroquine resistance; Malaria; Plasmodium.

MeSH terms

  • Animals
  • Antimalarials / therapeutic use*
  • Chloroquine / analogs & derivatives*
  • Chloroquine / therapeutic use*
  • Drug Resistance / drug effects
  • Humans
  • Malaria / drug therapy
  • Male
  • Mice
  • Parasitemia / drug therapy
  • Plasmodium berghei / drug effects*
  • Plasmodium falciparum / drug effects*

Substances

  • Antimalarials
  • Chloroquine