title: Synthesis and antikinetoplastid activities of 3-substituted quinolinones derivatives.
abstract: A new family of quinolinone derivatives has been synthesized and evaluated for their antikinetoplastid activities against Leishmania donovani and Trypanosoma brucei brucei. Results from these structure-activity relationship studies enabled identification of compounds 3a and 4g as the most active compounds against L. donovani promastigotes and amastigotes parasites (IC(50) values in a range of 2-11 μM). Additionally, compound 3b has emerged from this study as the most active compound in the series against T. b. brucei with a MEC value of 12 μM. These three compounds are worth of further in vivo evaluation.
authors.affiliation: Univ Paris-Sud, CNRS, BioCIS-UMR 8076, Laboratoire de Chimie Thérapeutique, LabEx LERMIT, Faculté de Pharmacie, 5 rue J.-B. Clément, Châtenay-Malabry, F-92296, France.
authors.forename: Davide
authors.initials: D
authors.lastname: Audisio
authors.forename: Samir
authors.initials: S
authors.lastname: Messaoudi
authors.forename: Sandrine
authors.initials: S
authors.lastname: Cojean
authors.forename: Jean-François
authors.initials: JF
authors.lastname: Peyrat
authors.forename: Jean-Daniel
authors.initials: JD
authors.lastname: Brion
authors.forename: Christian
authors.initials: C
authors.lastname: Bories
authors.forename: Françoise
authors.initials: F
authors.lastname: Huteau
authors.forename: Philippe M
authors.initials: PM
authors.lastname: Loiseau
authors.forename: Mouad
authors.initials: M
authors.lastname: Alami
mesh_terms: D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D015195:Drug Design; D007893:Leishmania donovani / Q000187:drug effects*; D051379:Mice; D015363:Quinolones / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology* / Q000633:toxicity; D013329:Structure-Activity Relationship; D014346:Trypanosoma brucei brucei / Q000187:drug effects*
chemical_list: D000981:Antiprotozoal Agents; D015363:Quinolones