2-Aminotetralones: Novel inhibitors of MurA and MurZ

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DUNSMORE, C. J., MILLER, K., BLAKE, K. L., PATCHING, S. G., HENDERSON, P. J. F., GARNETT, J. A., STUBBINGS, W. J., PHILLIPS, S. E. V., PALESTRANT, D. J. and ANGELES, J. de L. (2008). 2-Aminotetralones: Novel inhibitors of MurA and MurZ. Bioorganic & Medicinal Chemistry Letters, 18 (5), 1730-1734. [Article]

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Abstract

Several 2-aminotetralones were identified as novel inhibitors of the bacterial enzymes MurA and MurZ. A number of these inhibitors demonstrated antibacterial activity against Staphylococcus aureus and Escherichia coli with MICs in the range 8-128 microg/ml. Based on structure-activity relationships we propose that the alpha-aminoketone functionality is responsible for the inhibitory activity and evidence is provided to support a covalent mode of action involving the C115 thiol group of MurA/MurZ.

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Research Institute, Centre or Group - Does NOT include content added after October 2018:

Biomedical Research Centre

Page Range:

1730-1734

Identifiers

Identification Number:

10.1016/j.bmcl.2008.01.089

ORCID:

https://orcid.org/0000-0001-8633-6952