title: Design, synthesis and antimalarial activity of a glyoxylylhydrazone library.
abstract: Synthesis of a new family of quinolylhydrazone derivatives and evaluation of their activity against a chloroquine-resistant strain of Plasmodium falciparum are described. The best compound displayed an activity 6-fold higher than chloroquine. None of the active compounds were found to inhibit beta-hematin formation in vitro in the same range as chloroquine and five among them displayed lower calculated vacuolar accumulation ratios, suggesting the implication of a different mechanism of action.
authors.affiliation: Institut de Biologie et Institut Pasteur de Lille--UMR CNRS 8525--Université de Lille II, 1 rue du Professeur Calmette, BP 447, 59021, France.
authors.forename: A
authors.initials: A
authors.lastname: Ryckebusch
authors.forename: J-S
authors.initials: JS
authors.lastname: Fruchart
authors.forename: L
authors.initials: L
authors.lastname: Cattiaux
authors.forename: P
authors.initials: P
authors.lastname: Rousselot-Paillet
authors.forename: V
authors.initials: V
authors.lastname: Leroux
authors.forename: O
authors.initials: O
authors.lastname: Melnyk
authors.forename: P
authors.initials: P
authors.lastname: Grellier
authors.forename: E
authors.initials: E
authors.lastname: Mouray
authors.forename: C
authors.initials: C
authors.lastname: Sergheraert
authors.forename: P
authors.initials: P
authors.lastname: Melnyk
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000138:chemical synthesis* / Q000494:pharmacology; D006038:Glyoxylates / Q000138:chemical synthesis* / Q000494:pharmacology; D006835:Hydrazones / Q000138:chemical synthesis* / Q000494:pharmacology; D010963:Plasmodium falciparum / Q000187:drug effects / Q000254:growth & development
chemical_list: D000962:Antimalarials; D006038:Glyoxylates; D006835:Hydrazones; C031150:glyoxylic acid