High-throughput screening of metal-N-heterocyclic carbene complexes against biofilm formation by pathogenic bacteria

ChemMedChem. 2014 Jun;9(6):1140-4. doi: 10.1002/cmdc.201402012. Epub 2014 Apr 11.

Abstract

A set of molecules including a majority of metal-N-heterocyclic carbene (NHC) complexes (metal=Ag, Cu, and Au) and azolium salts were evaluated by high-throughput screening of their activity against biofilm formation associated with pathogenic bacteria. The anti-planktonic effects were compared in parallel. Representative biofilm-forming strains of various genera were selected (Listeria, Pseudomonas, Staphylococcus, and Escherichia). All the compounds were tested at 1 mg L(-1) by using the BioFilm Ring Test. An information score (IS, sum of the activities) and an activity score (AS, difference between anti-biofilm and anti-planktonic activity) were determined from normalized experimental values to classify the most active molecules against the panel of bacterial strains. With this method we identified lipophilic Ag(I) and Cu(I) complexes possessing aromatic groups on the NHC ligand as the most efficient at inhibiting biofilm formation.

Keywords: antibiotics; biofilms; carbene ligands; group 11 elements; high-throughput screening.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Bacterial Agents / chemistry*
  • Anti-Bacterial Agents / pharmacology
  • Biofilms / drug effects*
  • Biofilms / growth & development
  • Coordination Complexes / chemistry*
  • Coordination Complexes / pharmacology
  • Copper / chemistry
  • Gold / chemistry
  • Gram-Negative Bacteria / physiology
  • Gram-Positive Bacteria / physiology
  • Heterocyclic Compounds / chemistry*
  • Methane / analogs & derivatives*
  • Methane / chemistry
  • Microbial Sensitivity Tests
  • Silver / chemistry

Substances

  • Anti-Bacterial Agents
  • Coordination Complexes
  • Heterocyclic Compounds
  • carbene
  • Silver
  • Gold
  • Copper
  • Methane