4.6 Article

Evaluation of Ruthenium(II) N-Heterocyclic Carbene Complexes as Antibacterial Agents and Inhibitors of Bacterial Thioredoxin Reductase

Journal

MOLECULES
Volume 26, Issue 14, Pages -

Publisher

MDPI
DOI: 10.3390/molecules26144282

Keywords

antibacterial; N-heterocyclic carbenes; ruthenium; thioredoxin reductase

Funding

  1. Lower Saxony Ministry for Science and Culture for the doctoral program Drug Discovery and Cheminformatics for New Anti-Infectives (iCA)
  2. German Federal State of North Rhine-Westphalia
  3. European Union, European Regional Development Fund, Investing in Your Future for the Research Infrastructure Center for System-Based Antibiotic Research (CESAR)

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Ruthenium(II) NHC complexes exhibited stronger antibacterial effects compared to metal-free benzimidazolium cations, particularly against Gram-positive bacteria. The inhibition of bacterial thioredoxin reductase by selected complexes suggested a potential contributing factor to their antibacterial effects.
A series of ruthenium(II) complexes with N-heterocyclic carbene (NHC) ligands of the general type (arene)(NHC)Ru(II)X-2 (where X = halide) was prepared, characterized, and evaluated as antibacterial agents in comparison to the respective metal free benzimidazolium cations. The ruthenium(II) NHC complexes generally triggered stronger bacterial growth inhibition than the metal free benzimidazolium cations. The effects were much stronger against Gram-positive bacteria (Bacillus subtilis and Staphylococcus aureus) than against Gram-negative bacteria (Escherichia coli, Acinetobacter baumannii, Pseudomonas aeruginosa), and all complexes were inactive against the fungus Candida albicans. Moderate inhibition of bacterial thioredoxin reductase was confirmed for selected complexes, indicating that inhibition of this enzyme might be a contributing factor to the antibacterial effects.

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