title: Derivatives of 8-hydroxyquinoline--antibacterial agents that target intra- and extracellular Gram-negative pathogens.
abstract: Small molecule screening identified 5-nitro-7-((4-phenylpiperazine-1-yl-)methyl)quinolin-8-ol INP1750 as a putative inhibitor of type III secretion (T3S) in the Gram-negative pathogen Yersinia pseudotuberculosis. In this study we report structure-activity relationships for inhibition of T3S and show that the most potent compounds target both the extracellular bacterium Y. pseudotuberculosis and the intracellular pathogen Chlamydia trachomatis in cell-based infection models.
authors.affiliation: Laboratories for Chemical Biology Umeå, Department of Chemistry, Umeå University, Umeå, Sweden.
authors.forename: Per-Anders
authors.initials: PA
authors.lastname: Enquist
authors.forename: Asa
authors.initials: A
authors.lastname: Gylfe
authors.forename: Ulrik
authors.initials: U
authors.lastname: Hägglund
authors.forename: Pia
authors.initials: P
authors.lastname: Lindström
authors.forename: Henrik
authors.initials: H
authors.lastname: Norberg-Scherman
authors.forename: Charlotta
authors.initials: C
authors.lastname: Sundin
authors.forename: Mikael
authors.initials: M
authors.lastname: Elofsson
mesh_terms: D000900:Anti-Bacterial Agents / Q000494:pharmacology*; D006090:Gram-Negative Bacteria / Q000187:drug effects*; D006367:HeLa Cells; D006801:Humans; D015125:Oxyquinoline / Q000494:pharmacology*
chemical_list: D000900:Anti-Bacterial Agents; D015125:Oxyquinoline