Cargando…
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...
Autores principales: | , , , , , |
---|---|
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 |
_version_ | 1784749000293875712 |
---|---|
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. |
format | Online Article Text |
id | pubmed-9290826 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2021 |
publisher | John Wiley and Sons Inc. |
record_format | MEDLINE/PubMed |
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 |
work_keys_str_mv | AT bussingrolf goldiandgoldiiinheterocycliccarbenecomplexesasantibacterialagentsandinhibitorsofbacterialthioredoxinreductase AT kargebianka goldiandgoldiiinheterocycliccarbenecomplexesasantibacterialagentsandinhibitorsofbacterialthioredoxinreductase AT lippmannpetra goldiandgoldiiinheterocycliccarbenecomplexesasantibacterialagentsandinhibitorsofbacterialthioredoxinreductase AT jonespeterg goldiandgoldiiinheterocycliccarbenecomplexesasantibacterialagentsandinhibitorsofbacterialthioredoxinreductase AT bronstrupmark goldiandgoldiiinheterocycliccarbenecomplexesasantibacterialagentsandinhibitorsofbacterialthioredoxinreductase AT ottingo goldiandgoldiiinheterocycliccarbenecomplexesasantibacterialagentsandinhibitorsofbacterialthioredoxinreductase |