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

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• 作者：Brian Le贸n ; Jiunn C. N. Fong ; Kelly C. Peach ; Weng Ruh Wong ; Fitnat H. Yildiz ; Roger G. Linington
• 刊名：Organic Letters
• 出版年：2013
• 出版时间：March 15, 2013
• 年：2013
• 卷：15
• 期：6
• 页码：1234-1237
• 全文大小：310K
• 年卷期：v.15,no.6(March 15, 2013)
• ISSN：1523-7052

文摘

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鈥揾alogen exchange chemistry installed both stereocenters in one step, to afford a simpler scaffold than the initial lead molecule, with an EC₅₀ < 10 渭M.