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2-Aminotetralones: novel inhibitors of MurA and MurZ.

Dunsmore, Colin J and Miller, Keith and Blake, Katy L and Patching, Simon G and Henderson, Peter J F and Garnett, James and Stubbings, William J and Phillips, Simon E V and Palestrant, Deborah and De Los Angeles, Joseph and Leeds, Jennifer and 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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Additional Information: author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used
Keywords: 2-Aminotetralone; MurA inhibitor; MurZ inhibitor; Antibacterial activity
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Date Deposited: 14 Dec 2009 13:51
Last Modified: 31 Jan 2013 01:03
URI: https://oak.novartis.com/id/eprint/909

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