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Issue 4, 2017
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Microwave-enhanced Friedländer synthesis for the rapid assembly of halogenated quinolines with antibacterial and biofilm eradication activities against drug resistant and tolerant bacteria

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Abstract

Herein, we disclose the development of a catalyst- and protecting-group-free microwave-enhanced Friedländer synthesis which permits the single-step, convergent assembly of diverse 8-hydroxyquinolines with greatly improved reaction yields over traditional oil bath heating (increased from 34% to 72%). This rapid synthesis permitted the discovery of novel biofilm-eradicating halogenated quinolines (MBECs = 1.0–23.5 μM) active against MRSA, MRSE, and VRE. These small molecules exhibit activity through mechanisms independent of membrane lysis, further demonstrating their potential as a clinically useful treatment option against persistent biofilm-associated infections.

Graphical abstract: Microwave-enhanced Friedländer synthesis for the rapid assembly of halogenated quinolines with antibacterial and biofilm eradication activities against drug resistant and tolerant bacteria

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Publication details

The article was received on 08 Jul 2016, accepted on 25 Jul 2016 and first published on 27 Jul 2016


Article type: Research Article
DOI: 10.1039/C6MD00381H
Citation: Med. Chem. Commun., 2017,8, 720-724
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    Microwave-enhanced Friedländer synthesis for the rapid assembly of halogenated quinolines with antibacterial and biofilm eradication activities against drug resistant and tolerant bacteria

    A. T. Garrison, Y. Abouelhassan, H. Yang, H. H. Yousaf, T. J. Nguyen and R. W. Huigens III, Med. Chem. Commun., 2017, 8, 720
    DOI: 10.1039/C6MD00381H

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