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


Journal

Molecules (Basel, Switzerland)
ISSN: 1420-3049
Titre abrégé: Molecules
Pays: Switzerland
ID NLM: 100964009

Informations de publication

Date de publication:
13 Mar 2020
Historique:
received: 15 02 2020
revised: 05 03 2020
accepted: 09 03 2020
entrez: 19 3 2020
pubmed: 19 3 2020
medline: 17 12 2020
Statut: epublish

Résumé

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,

Identifiants

pubmed: 32183087
pii: molecules25061315
doi: 10.3390/molecules25061315
pmc: PMC7145296
pii:
doi:

Substances chimiques

Enzyme Inhibitors 0
Oligopeptides 0
Tetrazoles 0
Alanine Racemase EC 5.1.1.1

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Subventions

Organisme : bioMerieux
ID : n/a

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Auteurs

Laszlo A Kondacs (LA)

Sunderland Pharmacy School, University of Sunderland, Sunderland SR1 3SD, UK.

Sylvain Orenga (S)

Research & Development Microbiology, bioMérieux, 38390 La Balme-les-Grottes, France.

Rosaleen J Anderson (RJ)

Sunderland Pharmacy School, University of Sunderland, Sunderland SR1 3SD, UK.

Emma C L Marrs (ECL)

Department of Microbiology, Freeman Hospital, Newcastle upon Tyne NE7 7DN, UK.

John D Perry (JD)

Department of Microbiology, Freeman Hospital, Newcastle upon Tyne NE7 7DN, UK.

Mark Gray (M)

Sunderland Pharmacy School, University of Sunderland, Sunderland SR1 3SD, UK.

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Classifications MeSH