Derivatives of 8-hydroxyquinoline--antibacterial agents that target intra- and extracellular Gram-negative pathogens.

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Enquist P, Gylfe A, Hägglund U, Lindström P, Norberg-Scherman H, Sundin C, Elofsson M

Bioorg. Med. Chem. Lett. 22 (10) 3550-3553 [2012-05-15; online 2012-04-25]

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.

Chemical Biology Consortium Sweden (CBCS) [Collaborative]

PubMed 22525317

DOI 10.1016/j.bmcl.2012.03.096

Crossref 10.1016/j.bmcl.2012.03.096

pii: S0960-894X(12)00426-X

Laboratories for Chemical Biology Umeå (LCBU)