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Issue 6, 2013
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Indoletriazole conjugates are selective inhibitors and inducers of bacterial biofilms

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Abstract

Herein is described a method of accessing indoletriazole and benzothiophenetriazole analogues that selectively promote or inhibit biofilm formation by Gram-positive and Gram-negative bacteria. Structure/function studies revealed that the addition of a bromine atom at the 2-position of the indole–triazole scaffold altered activity against both Gram-negative and Gram-positive bacteria and could transform a biofilm inhibitor into a biofilm inducer. Isosteric replacement of the indole core by a benzothiophene significantly impaired anti-biofilm activity. A competition assay exposing Escherichia coli to the most potent biofilm inducer and an inhibitor of E. coli biofilm formation was performed. The inducer exhibited the ability to mute the effect of the anti-biofilm compound for this targeted bacterial population.

Graphical abstract: Indole–triazole conjugates are selective inhibitors and inducers of bacterial biofilms

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Publication details

The article was received on 26 Feb 2013, accepted on 05 Apr 2013 and first published on 16 Apr 2013


Article type: Concise Article
DOI: 10.1039/C3MD00064H
Med. Chem. Commun., 2013,4, 916-919

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    Indoletriazole conjugates are selective inhibitors and inducers of bacterial biofilms

    M. J. Minvielle, C. A. Bunders and C. Melander, Med. Chem. Commun., 2013, 4, 916
    DOI: 10.1039/C3MD00064H

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