title: In vitro chemosensitivity of Plasmodium falciparum to four chloroquine derivatives.
abstract: The antimalarial activity of four chloroquine derivatives has been assessed in vitro by the Trager and Jensen technique against the strain of Plasmodium falciparum FCC, 2spp. Monodesethyl-chloroquine possessed a significant activity, reducing the parasitaemia to 5% with 2 nM ml-1 (base). The hydroxy-metabolite showed a slight activity, reducing the parasitaemia to 39.5% with 2 nM ml-1 (base). No activity was found with the amino-metabolite and the pyrrolidinyl chemical derivative. The anti-malarial activity of monodesethyl-chloroquine should be considered for pharmacokinetics and for optimizing chloroquine treatments.
authors.affiliation: Faculté de Pharmacie, Marseille, France.
authors.forename: M
authors.initials: M
authors.lastname: Gasquet
authors.forename: A
authors.initials: A
authors.lastname: Atouk
authors.forename: A
authors.initials: A
authors.lastname: Samat
authors.forename: P
authors.initials: P
authors.lastname: Timon-David
authors.forename: A
authors.initials: A
authors.lastname: Viala
mesh_terms: D000818:Animals; D002738:Chloroquine / Q000031:analogs & derivatives* / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D010963:Plasmodium falciparum / Q000187:drug effects*
chemical_list: D002738:Chloroquine; C007278:desethylchloroquine