O'Beirne, Cillian, Piatek, Magdalena E, Fossen, Jen, Müller-Bunz, Helge, Andes, David R, Kavanagh, Kevin, Patil, Siddappa A, Baumann, Marcus and Tacke, Matthias (2020) Continuous flow synthesis and antimicrobial evaluation of NHC* silver carboxylate derivatives of SBC3 in vitro and in vivo. Metallomics, 13 (2). ISSN 1756-591X
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Abstract
N-heterocyclic silver carbene compounds have been extensively studied and shown to be active agents against a host of pathogenic bacteria and fungi. By incorporating hypothesized virulence targeting substituents into NHC–silver systems via salt metathesis, an atom-efficient complexation process can be used to develop new complexes to target the passive and active systems of a microbial cell.
The incorporation of fatty acids and an FtsZ inhibitor have been achieved, and creation of both the intermediate salt and subsequent silver complex has been streamlined into a continuous flow process. Biological evaluation was conducted with in vitro toxicology assays showing these novel complexes had excellent inhibition against Gram-negative strains E. coli, P. aeruginosa, and K. pneumoniae;
further studies also confirmed the ability to inhibit biofilm formation in methicillin-resistant Staphylococcus aureus (MRSA) and C. Parapsilosis. In vivo testing using a murine thigh infection model showed promising inhibition of MRSA for the lead compound SBC3, which is derived from 1,3-dibenzyl-4,5-diphenylimidazol-2-ylidene (NHC*
Item Type: | Article |
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Additional Information: | Cite as: O'Beirne, C., Piatek, M.E., Fossen, J., Müller-Bunz, H., Andes, D.R., Kavanagh, K., Patil, S.A., Baumann, M. & Tacke, M. 2021, "Continuous flow synthesis and antimicrobial evaluation of NHC silver carboxylate derivatives of SBC3 in vitro and in vivo", Metallomics, vol. 13, no. 2 |
Keywords: | antimicrobial agents; in vitro; SBC3; |
Academic Unit: | Faculty of Science and Engineering > Biology Faculty of Science and Engineering > Research Institutes > Human Health Institute |
Item ID: | 17301 |
Identification Number: | 10.1093/mtomcs/mfaa011 |
Depositing User: | Dr. Kevin Kavanagh |
Date Deposited: | 08 Jun 2023 14:52 |
Journal or Publication Title: | Metallomics |
Publisher: | Oxford |
Refereed: | Yes |
Related URLs: | |
URI: | https://mural.maynoothuniversity.ie/id/eprint/17301 |
Use Licence: | This item is available under a Creative Commons Attribution Non Commercial Share Alike Licence (CC BY-NC-SA). Details of this licence are available here |
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