title: Design, synthesis and in vitro antikinetoplastid evaluation of N-acylated putrescine, spermidine and spermine derivatives.
abstract: A structure-activity relationship study on polyamine derivatives led to the synthesis and the determination of antikinetoplastid activity of 17 compounds. Among them, a spermidine derivative (compound 13) was specifically active in vitro against Leishmania donovani axenic amastigotes (IC50 at 5.4μM; Selectivity Index >18.5) and a spermine derivative (compound 28) specifically active against Trypanosoma brucei gambiense (IC50 at 1.9μM; Selectivity Index >52).
authors.affiliation: Chimie Bioorganique et Bioinorganique, LabEx LERMIT, CNRS, UMR 8182 (ICMMO), Bâtiment 420, Université Paris-Sud, 15 rue Georges Clemenceau, 91405 Orsay cedex, France.
authors.forename: Elodie
authors.initials: E
authors.lastname: Jagu
authors.affiliation: Chimie Bioorganique et Bioinorganique, LabEx LERMIT, CNRS, UMR 8182 (ICMMO), Bâtiment 420, Université Paris-Sud, 15 rue Georges Clemenceau, 91405 Orsay cedex, France.
authors.forename: Rachid
authors.initials: R
authors.lastname: Djilali
authors.affiliation: Chimiothérapie Antiparasitaire, LabEx LERMIT, Faculté de Pharmacie, CNRS, UMR 8076 (BioCIS), Université Paris-Sud, 5 rue Jean-Baptiste Clément, 92290 Châtenay-Malabry, France.
authors.forename: Sébastien
authors.initials: S
authors.lastname: Pomel
authors.affiliation: Chimie Bioorganique et Bioinorganique, LabEx LERMIT, CNRS, UMR 8182 (ICMMO), Bâtiment 420, Université Paris-Sud, 15 rue Georges Clemenceau, 91405 Orsay cedex, France.
authors.forename: Florence
authors.initials: F
authors.lastname: Ramiandrasoa
authors.affiliation: Chimie Bioorganique et Bioinorganique, LabEx LERMIT, CNRS, UMR 8182 (ICMMO), Bâtiment 420, Université Paris-Sud, 15 rue Georges Clemenceau, 91405 Orsay cedex, France.
authors.forename: Stéphanie
authors.initials: S
authors.lastname: Pethe
authors.affiliation: Chimie Bioorganique et Bioinorganique, LabEx LERMIT, CNRS, UMR 8182 (ICMMO), Bâtiment 420, Université Paris-Sud, 15 rue Georges Clemenceau, 91405 Orsay cedex, France. Electronic address: raphael.labruere@u-psud.fr.
authors.forename: Raphaël
authors.initials: R
authors.lastname: Labruère
authors.affiliation: Chimiothérapie Antiparasitaire, LabEx LERMIT, Faculté de Pharmacie, CNRS, UMR 8076 (BioCIS), Université Paris-Sud, 5 rue Jean-Baptiste Clément, 92290 Châtenay-Malabry, France. Electronic address: philippe.loiseau@u-psud.fr.
authors.forename: Philippe M
authors.initials: PM
authors.lastname: Loiseau
authors.affiliation: Chimie Bioorganique et Bioinorganique, LabEx LERMIT, CNRS, UMR 8182 (ICMMO), Bâtiment 420, Université Paris-Sud, 15 rue Georges Clemenceau, 91405 Orsay cedex, France. Electronic address: casimir.blonski@u-psud.fr.
authors.forename: Casimir
authors.initials: C
authors.lastname: Blonski
mesh_terms: D000215:Acylation; D000981:Antiprotozoal Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D015195:Drug Design; D004353:Drug Evaluation, Preclinical / Q000379:methods; D016830:Kinetoplastida / Q000187:drug effects*; D007893:Leishmania donovani / Q000187:drug effects; D011700:Putrescine / Q000138:chemical synthesis* / Q000494:pharmacology; D013095:Spermidine / Q000138:chemical synthesis* / Q000494:pharmacology; D013096:Spermine / Q000138:chemical synthesis* / Q000494:pharmacology; D014346:Trypanosoma brucei brucei / Q000187:drug effects
chemical_list: D000981:Antiprotozoal Agents; D013096:Spermine; D013095:Spermidine; D011700:Putrescine
keywords: Antikinetoplastids; Leishmania donovani; Polyamines; Trypanosoma brucei