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C-Terminal 1-Aminoethyltetrazole-Containing Oligopeptides as Novel Alanine Racemase Inhibitors

Kondacs, Laszlo A., Orenga, Sylvain, Anderson, Rosaleen, Marrs, Emma C.L., Perry, John D. and Gray, Mark (2020) C-Terminal 1-Aminoethyltetrazole-Containing Oligopeptides as Novel Alanine Racemase Inhibitors. Molecules, 25 (6). e1315. ISSN 1420-3049

Item Type: Article

Abstract

In clinical culture media inoculated with patient samples, selective inhibition of commensal bacteria is essential for accurate diagnosis and effective treatment, as they can mask the presence of pathogenic bacteria. The alanine analogue, 1-aminoethyltetrazole was investigated as a potential alanine racemase inhibitor. For effective uptake and enhanced and selective antibacterial activity, a library of C-terminal 1-aminoethyltetrazole containing di- and oligopeptides were synthesized by solid phase peptide coupling techniques. The investigation of the antimicrobial activity of the synthesised compounds identified several clinically applicable selective inhibitors. These enabled differentiation between the closely related bacteria, Salmonella and Escherichia coli, which can be difficult to discriminate between in a clinical setting. In addition, differentiation between enterococci and other Gram-positive cocci was also seen.

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Additional Information: ** From MDPI via Jisc Publications Router ** History: accepted 09-03-2020; pub-electronic 13-03-2020. ** Licence for this article: https://creativecommons.org/licenses/by/4.0/
Uncontrolled Keywords: alanine racemase, 1-aminoethyltetrazole, antibacterial agent, selective inhibition, solid phase peptide synthesis
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Depositing User: Publication Router

Identifiers

Item ID: 11864
Identification Number: https://doi.org/10.3390/molecules25061315
ISSN: 1420-3049
URI: http://sure.sunderland.ac.uk/id/eprint/11864
Official URL: https://www.mdpi.com/1420-3049/25/6/1315

Users with ORCIDS

ORCID for Laszlo A. Kondacs: ORCID iD orcid.org/0000-0001-5529-2061
ORCID for Mark Gray: ORCID iD orcid.org/0000-0002-0674-1999

Catalogue record

Date Deposited: 25 Mar 2020 09:47
Last Modified: 05 Feb 2021 11:51

Contributors

Author: Laszlo A. Kondacs ORCID iD
Author: Mark Gray ORCID iD
Author: Sylvain Orenga
Author: Rosaleen Anderson
Author: Emma C.L. Marrs
Author: John D. Perry

University Divisions

Faculty of Health Sciences and Wellbeing > School of Pharmacy and Pharmaceutical Sciences

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