Dunsmore, Colin J, Miller, Keith, Blake, Katy L, Patching, Simon G, Henderson, Peter J F, Garnett, James, Stubbings, William J, Phillips, Simon E V, Palestrant, Deborah, De Los Angeles, Joseph, Leeds, Jennifer, 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
Related URLs:	http://www.ncbi.nlm.nih.gov/sites/entrez...
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
Related URLs:	http://www.ncbi.nlm.nih.gov/sites/entrez...
Date Deposited:	14 Dec 2009 13:51
Last Modified:	31 Jan 2013 01:03
URI:	https://oak.novartis.com/id/eprint/909