Development of Quinoline-Based Disruptors of Biofilm Formation Against Vibrio cholerae

Biofilm formation is a major cause of bacterial persistence in nosocomial infections, leading to extended treatment times and increased rates of morbidity and mortality. Despite this, there are currently no biofilm inhibitors approved for clinical use. The synthesis and biological evaluation of a li...

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Veröffentlicht in:Organic letters 2013-03, Vol.15 (6), p.1234-1237
Hauptverfasser: León, Brian, Fong, Jiunn C. N, Peach, Kelly C, Wong, Weng Ruh, Yildiz, Fitnat H, Linington, Roger G
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Sprache:eng
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Zusammenfassung:Biofilm formation is a major cause of bacterial persistence in nosocomial infections, leading to extended treatment times and increased rates of morbidity and mortality. Despite this, there are currently no biofilm inhibitors approved for clinical use. The synthesis and biological evaluation of a library of amino alcohol quinolines as lead compounds for the disruption of biofilm formation in Vibrio cholerae is now reported. Application of selective metal–halogen exchange chemistry installed both stereocenters in one step, to afford a simpler scaffold than the initial lead molecule, with an EC50 < 10 μM.
ISSN:1523-7060
1523-7052
DOI:10.1021/ol400150z