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Investigations into the Antibacterial Activity of the Silver-Based Antibiotic Drug Candidate SBC3

The synthesis of N-heterocyclic carbene (NHC) silver(I) acetate complexes with varying lipophilic benzyl-substituents at the 1 and 3 positions starting from 4,5-diphenylimidazole, opened a new class of antibiotic drug candidates. These NHC-silver(I) acetate derivatives exhibit interesting structural...

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Autores principales: Sharkey, Michael A., O’Gara, James P., Gordon, Stephen V., Hackenberg, Frauke, Healy, Claire, Paradisi, Francesca, Patil, Siddappa, Schaible, Bettina, Tacke, Matthias
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2012
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4790244/
http://dx.doi.org/10.3390/antibiotics1010025
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author Sharkey, Michael A.
O’Gara, James P.
Gordon, Stephen V.
Hackenberg, Frauke
Healy, Claire
Paradisi, Francesca
Patil, Siddappa
Schaible, Bettina
Tacke, Matthias
author_facet Sharkey, Michael A.
O’Gara, James P.
Gordon, Stephen V.
Hackenberg, Frauke
Healy, Claire
Paradisi, Francesca
Patil, Siddappa
Schaible, Bettina
Tacke, Matthias
author_sort Sharkey, Michael A.
collection PubMed
description The synthesis of N-heterocyclic carbene (NHC) silver(I) acetate complexes with varying lipophilic benzyl-substituents at the 1 and 3 positions starting from 4,5-diphenylimidazole, opened a new class of antibiotic drug candidates. These NHC-silver(I) acetate derivatives exhibit interesting structural motifs in the solid state and proved to be soluble and stable in biological media. The leading candidate, SBC3, which was known to exhibit good antibacterial activity in preliminary Kirby-Bauer tests, was tested quantitatively using minimum inhibitory concentrations. NHC-silver(I) acetate complexes were found to have MIC values ranging from 20 to 3.13 μg/mL for a variety of Gram-positive, Gram-negative and mycobacteria tested. These values represent good antibiotic activities against potential pathogens when compared to clinically approved antibiotics. Most striking is the fact that SBC3 is active against methicillin-resistant Staphylococcus aureus with a MIC value of 12.5 μg/mL.
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spelling pubmed-47902442016-03-24 Investigations into the Antibacterial Activity of the Silver-Based Antibiotic Drug Candidate SBC3 Sharkey, Michael A. O’Gara, James P. Gordon, Stephen V. Hackenberg, Frauke Healy, Claire Paradisi, Francesca Patil, Siddappa Schaible, Bettina Tacke, Matthias Antibiotics (Basel) Short Note The synthesis of N-heterocyclic carbene (NHC) silver(I) acetate complexes with varying lipophilic benzyl-substituents at the 1 and 3 positions starting from 4,5-diphenylimidazole, opened a new class of antibiotic drug candidates. These NHC-silver(I) acetate derivatives exhibit interesting structural motifs in the solid state and proved to be soluble and stable in biological media. The leading candidate, SBC3, which was known to exhibit good antibacterial activity in preliminary Kirby-Bauer tests, was tested quantitatively using minimum inhibitory concentrations. NHC-silver(I) acetate complexes were found to have MIC values ranging from 20 to 3.13 μg/mL for a variety of Gram-positive, Gram-negative and mycobacteria tested. These values represent good antibiotic activities against potential pathogens when compared to clinically approved antibiotics. Most striking is the fact that SBC3 is active against methicillin-resistant Staphylococcus aureus with a MIC value of 12.5 μg/mL. MDPI 2012-11-20 /pmc/articles/PMC4790244/ http://dx.doi.org/10.3390/antibiotics1010025 Text en © 2012 by the authors; licensee MDPI, Basel, Switzerland. This article is an open-access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Short Note
Sharkey, Michael A.
O’Gara, James P.
Gordon, Stephen V.
Hackenberg, Frauke
Healy, Claire
Paradisi, Francesca
Patil, Siddappa
Schaible, Bettina
Tacke, Matthias
Investigations into the Antibacterial Activity of the Silver-Based Antibiotic Drug Candidate SBC3
title Investigations into the Antibacterial Activity of the Silver-Based Antibiotic Drug Candidate SBC3
title_full Investigations into the Antibacterial Activity of the Silver-Based Antibiotic Drug Candidate SBC3
title_fullStr Investigations into the Antibacterial Activity of the Silver-Based Antibiotic Drug Candidate SBC3
title_full_unstemmed Investigations into the Antibacterial Activity of the Silver-Based Antibiotic Drug Candidate SBC3
title_short Investigations into the Antibacterial Activity of the Silver-Based Antibiotic Drug Candidate SBC3
title_sort investigations into the antibacterial activity of the silver-based antibiotic drug candidate sbc3
topic Short Note
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4790244/
http://dx.doi.org/10.3390/antibiotics1010025
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