title: Synthesis and antimalarial activity of new analogues of amodiaquine.
abstract: In order to determine the real significance of the 4'-phenolic group in the antimalarial activity and/or cytotoxicity of amodiaquine (AQ), analogues for which this functionality was shifted or modified were synthesized. Good in vitro antimalarial activity was obtained for compounds unable to form intramolecular hydrogen bond. Among the compounds synthesized, new amino derivative 5 displayed the greatest selectivity index towards the most CQ-resistant strain tested and was active in mice infected by Plasmodium berghei.
authors.affiliation: UMR CNRS 8525, Université de Lille II, Institut Pasteur de Lille 1 rue du Professeur Calmette, B.P. 447, 59021 Lille cedex, France.
authors.forename: Sandrine
authors.initials: S
authors.lastname: Delarue-Cochin
authors.forename: Emilia
authors.initials: E
authors.lastname: Paunescu
authors.forename: Louis
authors.initials: L
authors.lastname: Maes
authors.forename: Elisabeth
authors.initials: E
authors.lastname: Mouray
authors.forename: Christian
authors.initials: C
authors.lastname: Sergheraert
authors.forename: Philippe
authors.initials: P
authors.lastname: Grellier
authors.forename: Patricia
authors.initials: P
authors.lastname: Melnyk
mesh_terms: D000655:Amodiaquine / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002460:Cell Line; D002851:Chromatography, High Pressure Liquid; D005260:Female; D006801:Humans; D006860:Hydrogen Bonding; D009682:Magnetic Resonance Spectroscopy; D051379:Mice; D010962:Plasmodium berghei / Q000187:drug effects
chemical_list: D000962:Antimalarials; D000655:Amodiaquine