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Derivatives of 8-hydroxyquinoline--antibacterial agents that target intra- and extracellular Gram-negative pathogens |
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| Authors: | Enquist Per-Anders Gylfe Asa Hägglund Ulrik Lindström Pia Norberg-Scherman Henrik Sundin Charlotta Elofsson Mikael |
| Affiliation: | 1. Laboratories for Chemical Biology Umeå, Department of Chemistry, Umeå University, SE90187 Umeå, Sweden;2. Umeå Centre for Microbial Research and Laboratories for Molecular Infection Medicine Sweden, Umeå University, SE90187 Umeå, Sweden;3. Clinical Microbiology, Umeå University, SE90187 Umeå, Sweden;4. Creative Antibiotics, Tvistevägen 48, SE90719 Umeå, Sweden |
| 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. |
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