Indole/triazole conjugates are selective inhibitors and inducers of bacterial biofilms.
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 exposingEscherichia colito the most potent biofilm inducer and an inhibitor ofE. colibiofilm formation was performed. The inducer exhibited the ability to mute the effect of the anti-biofilm compound for this targeted bacterial population.
Department of Chemistry, North Carolina State University, Raleigh, NC, 27695-8204, USA. ; Tel: +1 919-513-2960.
Marine J
MJ
Minvielle
Cynthia A
CA
Bunders
Christian
C
Melander