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Indole/triazole conjugates are selective inhibitors and inducers of bacterial biofilms.

ABSTRACT: Herein is described a method of accessing indole/triazole and benzothiophene/triazole 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.

SUBMITTER: Minvielle MJ

PROVIDER: S-EPMC3733276 | biostudies-other | 2013 Jun

REPOSITORIES: biostudies-other

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Indole/triazole conjugates are selective inhibitors and inducers of bacterial biofilms.

Minvielle Marine J MJ Bunders Cynthia A CA Melander Christian C

MedChemComm 20130601 6

Herein is described a method of accessing indole/triazole and benzothiophene/triazole 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 be ...[more]

PMID: 23930199

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