Dunsmore, Colin J, Miller, Keith, Blake, Katy L, Patching, Simon G, Henderson, Peter J F, Garnett, James A, Stubbings, William J, Phillips, Simon E V, Palestrant, Deborah J, Angeles, Joseph De Los, Leeds, Jennifer A, Chopra, Ian and Fishwick, Colin W G (2008) 2-Aminotetralones: novel inhibitors of MurA and MurZ. Bioorganic & medicinal chemistry letters, 18 (5). pp. 1730-1734. ISSN 1464-3405

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.

Item Type:	Article
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Date Deposited:	13 Oct 2015 13:14
Last Modified:	13 Oct 2015 13:14
URI:	https://oak.novartis.com/id/eprint/6637