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Gold(I) and Gold(III) N‐Heterocyclic Carbene Complexes as Antibacterial Agents and Inhibitors of Bacterial Thioredoxin Reductase

A series of (NHC)Au(I)Cl monocarbene complexes and their gold(III) analogues (NHC)Au(III)Cl(3) were prepared and investigated as antibacterial agents and inhibitors of bacterial TrxR. The complexes showed stronger antibacterial effects against the Gram‐positive MRSA and E. faecium strains than again...

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Autores principales: Büssing, Rolf, Karge, Bianka, Lippmann, Petra, Jones, Peter G., Brönstrup, Mark, Ott, Ingo
Formato: Online Artículo Texto
Lenguaje:English
Publicado: John Wiley and Sons Inc. 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9290826/
https://www.ncbi.nlm.nih.gov/pubmed/34268875
http://dx.doi.org/10.1002/cmdc.202100381
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author Büssing, Rolf
Karge, Bianka
Lippmann, Petra
Jones, Peter G.
Brönstrup, Mark
Ott, Ingo
author_facet Büssing, Rolf
Karge, Bianka
Lippmann, Petra
Jones, Peter G.
Brönstrup, Mark
Ott, Ingo
author_sort Büssing, Rolf
collection PubMed
description A series of (NHC)Au(I)Cl monocarbene complexes and their gold(III) analogues (NHC)Au(III)Cl(3) were prepared and investigated as antibacterial agents and inhibitors of bacterial TrxR. The complexes showed stronger antibacterial effects against the Gram‐positive MRSA and E. faecium strains than against several Gram‐negative bacteria. All complexes were efficient inhibitors of bacterial thioredoxin reductase, indicating that inhibition of this enzyme might be involved in their mechanism of action. The efficacy of gold(I) and gold(III) analogues was comparable in most of the assays. The cytotoxicity of the gold NHC compounds against cancer and human cells was overall weaker than the activity against the Gram‐positive bacteria, suggesting that their optimization as antibacterials warrants further investigation.
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spelling pubmed-92908262022-07-20 Gold(I) and Gold(III) N‐Heterocyclic Carbene Complexes as Antibacterial Agents and Inhibitors of Bacterial Thioredoxin Reductase Büssing, Rolf Karge, Bianka Lippmann, Petra Jones, Peter G. Brönstrup, Mark Ott, Ingo ChemMedChem Full Papers A series of (NHC)Au(I)Cl monocarbene complexes and their gold(III) analogues (NHC)Au(III)Cl(3) were prepared and investigated as antibacterial agents and inhibitors of bacterial TrxR. The complexes showed stronger antibacterial effects against the Gram‐positive MRSA and E. faecium strains than against several Gram‐negative bacteria. All complexes were efficient inhibitors of bacterial thioredoxin reductase, indicating that inhibition of this enzyme might be involved in their mechanism of action. The efficacy of gold(I) and gold(III) analogues was comparable in most of the assays. The cytotoxicity of the gold NHC compounds against cancer and human cells was overall weaker than the activity against the Gram‐positive bacteria, suggesting that their optimization as antibacterials warrants further investigation. John Wiley and Sons Inc. 2021-08-03 2021-11-19 /pmc/articles/PMC9290826/ /pubmed/34268875 http://dx.doi.org/10.1002/cmdc.202100381 Text en © 2021 The Authors. ChemMedChem published by Wiley-VCH GmbH https://creativecommons.org/licenses/by-nc/4.0/This is an open access article under the terms of the http://creativecommons.org/licenses/by-nc/4.0/ (https://creativecommons.org/licenses/by-nc/4.0/) License, which permits use, distribution and reproduction in any medium, provided the original work is properly cited and is not used for commercial purposes.
spellingShingle Full Papers
Büssing, Rolf
Karge, Bianka
Lippmann, Petra
Jones, Peter G.
Brönstrup, Mark
Ott, Ingo
Gold(I) and Gold(III) N‐Heterocyclic Carbene Complexes as Antibacterial Agents and Inhibitors of Bacterial Thioredoxin Reductase
title Gold(I) and Gold(III) N‐Heterocyclic Carbene Complexes as Antibacterial Agents and Inhibitors of Bacterial Thioredoxin Reductase
title_full Gold(I) and Gold(III) N‐Heterocyclic Carbene Complexes as Antibacterial Agents and Inhibitors of Bacterial Thioredoxin Reductase
title_fullStr Gold(I) and Gold(III) N‐Heterocyclic Carbene Complexes as Antibacterial Agents and Inhibitors of Bacterial Thioredoxin Reductase
title_full_unstemmed Gold(I) and Gold(III) N‐Heterocyclic Carbene Complexes as Antibacterial Agents and Inhibitors of Bacterial Thioredoxin Reductase
title_short Gold(I) and Gold(III) N‐Heterocyclic Carbene Complexes as Antibacterial Agents and Inhibitors of Bacterial Thioredoxin Reductase
title_sort gold(i) and gold(iii) n‐heterocyclic carbene complexes as antibacterial agents and inhibitors of bacterial thioredoxin reductase
topic Full Papers
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9290826/
https://www.ncbi.nlm.nih.gov/pubmed/34268875
http://dx.doi.org/10.1002/cmdc.202100381
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