title: Design and synthesis of 3-isoxazolidone derivatives as new Chlamydia trachomatis inhibitors.
abstract: Chlamydia trachomatis (Ct) is a bacterial human pathogen responsible for the development of trachoma, the worldwide infection leading to blindness, and is also a major cause of sexually transmitted diseases. As iron is an essential metabolite for this bacterium, iron depletion presents a promising strategy to limit Ct proliferation. The aim of this study is to synthesize 3-isoxazolidone derivatives bearing known chelating moieties in an attempt to develop new bactericidal anti-Chlamydiaceae molecules. We have investigated the paths by which these new compounds affect Ct serovar L2 development in HeLa cells, in the presence or absence of exogenously added iron. The iron-chelating properties of these molecules were also determined. Our data reveal important bactericidal effects which are distinguishable from those due to iron chelation.
authors.affiliation: Univ Paris Diderot, Sorbonne Paris Cité, ITODYS, UMR 7086, CNRS, 15 rue Jean-Antoine de Baïf, F-75205 Paris, France.
authors.forename: S
authors.initials: S
authors.lastname: Abdelsayed
authors.affiliation: Univ Paris Diderot, Sorbonne Paris Cité, ITODYS, UMR 7086, CNRS, 15 rue Jean-Antoine de Baïf, F-75205 Paris, France.
authors.forename: N T
authors.initials: NT
authors.lastname: Ha Duong
authors.affiliation: Univ Paris Diderot, Sorbonne Paris Cité, ITODYS, UMR 7086, CNRS, 15 rue Jean-Antoine de Baïf, F-75205 Paris, France.
authors.forename: J
authors.initials: J
authors.lastname: Hai
authors.affiliation: Univ Paris Diderot, Sorbonne Paris Cité, ITODYS, UMR 7086, CNRS, 15 rue Jean-Antoine de Baïf, F-75205 Paris, France.
authors.forename: M
authors.initials: M
authors.lastname: Hémadi
authors.affiliation: Univ Paris Diderot, Sorbonne Paris Cité, ITODYS, UMR 7086, CNRS, 15 rue Jean-Antoine de Baïf, F-75205 Paris, France.
authors.forename: J M
authors.initials: JM
authors.lastname: El Hage Chahine
authors.affiliation: Laboratory of Inflammation, Gestation and Autoimmunity, Institut Jacques Monod-UMR 7592, CNRS and University Paris Diderot, 15 rue Hélène Brion, 75205 Paris Cedex 13, France. Electronic address: philippe.verbeke@inserm.fr.
authors.forename: P
authors.initials: P
authors.lastname: Verbeke
authors.affiliation: Univ Paris Diderot, Sorbonne Paris Cité, ITODYS, UMR 7086, CNRS, 15 rue Jean-Antoine de Baïf, F-75205 Paris, France. Electronic address: serradji@univ-paris-diderot.fr.
authors.forename: N
authors.initials: N
authors.lastname: Serradji
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D002692:Chlamydia trachomatis / Q000187:drug effects*; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D006367:HeLa Cells; D006801:Humans; D007555:Isoxazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D051379:Mice; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D023303:Oxazolidinones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D007555:Isoxazoles; D023303:Oxazolidinones; C013075:3-isoxazolidone
keywords: 3-Isoxazolidone; Chlamydia trachomatis inhibitors; Iron