title: Antimalarial in-vivo activity of bis(9-amino-6-chloro-2-methoxyacridines).
abstract: In the fight against malaria, chemotherapy using bisacridines may represent an alternative method to overcoming chloroquine-resistance. Eight bis(9-amino-6-chloro-2-methoxyacridines), in which acridine moieties were linked by polyamines substituted with a side chain, were tested for their in-vivo activity upon mice infected by Plasmodium berghei. Three of the compounds revealed antimalarial activity but no relationship could be deduced from a comparison of in-vitro and in-vivo activities. N-alkylation of the central amino group generated toxicity and, therefore, only compounds N-acylated in this position can be selected as leads.
authors.affiliation: UMR 8525 CNRS-Université de Lille II-Institut de Biologie et Institut Pasteur de Lille, France.
authors.forename: S
authors.initials: S
authors.lastname: Girault
authors.forename: S
authors.initials: S
authors.lastname: Delarue
authors.forename: P
authors.initials: P
authors.lastname: Grellier
authors.forename: A
authors.initials: A
authors.lastname: Berecibar
authors.forename: L
authors.initials: L
authors.lastname: Maes
authors.forename: L
authors.initials: L
authors.lastname: Quirijnen
authors.forename: P
authors.initials: P
authors.lastname: Lemiere
authors.forename: M A
authors.initials: MA
authors.lastname: Debreu-Fontaine
authors.forename: C
authors.initials: C
authors.lastname: Sergheraert
mesh_terms: D000609:Aminoacridines / Q000494:pharmacology* / Q000627:therapeutic use; D000818:Animals; D000962:Antimalarials / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use; D002738:Chloroquine / Q000494:pharmacology / Q000627:therapeutic use; D005260:Female; D008288:Malaria / Q000188:drug therapy / Q000469:parasitology; D051379:Mice; D010962:Plasmodium berghei / Q000187:drug effects*
chemical_list: D000609:Aminoacridines; D000962:Antimalarials; C010847:9-amino-6-chloro-2-methoxyacridine; D002738:Chloroquine