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C2 Arylated Benzo[b]thiophene Derivatives as Staphylococcus aureus NorA Efflux Pump Inhibitors.
Liger, François; Bouhours, Pascale; Ganem-Elbaz, Carine; Jolivalt, Claude; Pellet-Rostaing, Stéphane; Popowycz, Florence; Paris, Jean-Marc; Lemaire, Marc.
Afiliación
  • Liger F; Equipe Catalyse Synthèse Environnement, CNRS-UMR 5246, L'Institut de Chimie et Biochimie Moléculaires et Supramoléculaires (ICBMS), 43 Bd. du 11 novembre 1918, 69622, Villeurbanne, France.
  • Bouhours P; Laboratoire Charles Friedel, CNRS-UMR 7223, Chimie ParisTech, 11 rue Pierre et Marie Curie, 75005, Paris, France.
  • Ganem-Elbaz C; Laboratoire Charles Friedel, CNRS-UMR 7223, Chimie ParisTech, 11 rue Pierre et Marie Curie, 75005, Paris, France.
  • Jolivalt C; Laboratoire Charles Friedel, CNRS-UMR 7223, Chimie ParisTech, 11 rue Pierre et Marie Curie, 75005, Paris, France.
  • Pellet-Rostaing S; Equipe Catalyse Synthèse Environnement, CNRS-UMR 5246, L'Institut de Chimie et Biochimie Moléculaires et Supramoléculaires (ICBMS), 43 Bd. du 11 novembre 1918, 69622, Villeurbanne, France.
  • Popowycz F; Institut National des Sciences Appliquées de Lyon, ICBMS, CNRS-UMR 5246, Equipe Chimie Organique et Bioorganique, 20 Avenue Albert Einstein, 69621, Villeurbanne, France. Florence.Popowycz@insa-lyon.fr.
  • Paris JM; Laboratoire Charles Friedel, CNRS-UMR 7223, Chimie ParisTech, 11 rue Pierre et Marie Curie, 75005, Paris, France. claude.jolivalt@upmc.fr.
  • Lemaire M; Equipe Catalyse Synthèse Environnement, CNRS-UMR 5246, L'Institut de Chimie et Biochimie Moléculaires et Supramoléculaires (ICBMS), 43 Bd. du 11 novembre 1918, 69622, Villeurbanne, France. marc.lemaire@univ-lyon1.fr.
ChemMedChem ; 11(3): 320-30, 2016 Feb 04.
Article en En | MEDLINE | ID: mdl-26732895
An innovative and straightforward synthesis of second-generation 2-arylbenzo[b]thiophenes as structural analogues of INF55 and the first generation of our laboratory-made molecules was developed. The synthesis of C2-arylated benzo[b]thiophene derivatives was achieved through a method involving direct arylation, followed by simple structural modifications. Among the 34 compounds tested, two of them were potent NorA pump inhibitors, which led to a 16-fold decrease in the ciprofloxacin minimum inhibitory concentration (MIC) against the SA-1199B strain at concentrations of 0.25 and 0.5 µg mL(-1) (1 and 1.5 µm, respectively). This is a promising result relative to that obtained for reserpine (MIC=20 µg mL(-1)), a reference compound amongst NorA pump inhibitors. These molecules thus represent promising candidates to be used in combination with ciprofloxacin against fluoroquinolone-resistant strains.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Staphylococcus / Tiofenos / Proteínas Bacterianas / Proteínas Asociadas a Resistencia a Múltiples Medicamentos / Antibacterianos Idioma: En Revista: ChemMedChem Asunto de la revista: FARMACOLOGIA / QUIMICA Año: 2016 Tipo del documento: Article País de afiliación: Francia Pais de publicación: Alemania
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Staphylococcus / Tiofenos / Proteínas Bacterianas / Proteínas Asociadas a Resistencia a Múltiples Medicamentos / Antibacterianos Idioma: En Revista: ChemMedChem Asunto de la revista: FARMACOLOGIA / QUIMICA Año: 2016 Tipo del documento: Article País de afiliación: Francia Pais de publicación: Alemania