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

Per-Anders Enquist; Asa Gylfe; Ulrik Hägglund; Pia Lindström; Henrik Norberg-Scherman; Charlotta Sundin; Mikael Elofsson

doi:10.1016/j.bmcl.2012.03.096

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

Bioorg Med Chem Lett. 2012 May 15;22(10):3550-3. doi: 10.1016/j.bmcl.2012.03.096. Epub 2012 Apr 6.

Authors

Per-Anders Enquist¹, Asa Gylfe, Ulrik Hägglund, Pia Lindström, Henrik Norberg-Scherman, Charlotta Sundin, Mikael Elofsson

Affiliation

¹ Laboratories for Chemical Biology Umeå, Department of Chemistry, Umeå University, Umeå, Sweden.

PMID: 22525317
DOI: 10.1016/j.bmcl.2012.03.096

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.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Anti-Bacterial Agents / pharmacology*
Gram-Negative Bacteria / drug effects*
HeLa Cells
Humans
Oxyquinoline / pharmacology*

Substances

Anti-Bacterial Agents
Oxyquinoline