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. 2008 Mar 1;18(5):1730-4.
doi: 10.1016/j.bmcl.2008.01.089. Epub 2008 Jan 30.

2-Aminotetralones: novel inhibitors of MurA and MurZ

Colin J Dunsmore  1 , Keith Miller, Katy L Blake, Simon G Patching, Peter J F Henderson, James A Garnett, William J Stubbings, Simon E V Phillips, Deborah J Palestrant, Joseph De Los Angeles, Jennifer A Leeds, Ian Chopra, Colin W G Fishwick
Affiliations

2-Aminotetralones: novel inhibitors of MurA and MurZ

Colin J Dunsmore et al. Bioorg Med Chem Lett. .

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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