King's College London

Research portal

2-Aminotetralones: Novel inhibitors of MurA and MurZ

Research output: Contribution to journalArticle

Colin J. Dunsmore, 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

Original languageEnglish
Pages (from-to)1730-1734
Number of pages5
JournalBIOORGANIC AND MEDICINAL CHEMISTRY LETTERS
Volume18
Issue number5
DOIs
Publication statusPublished - 1 Mar 2008

King's Authors

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 μg/ml. Based on structure-activity relationships we propose that the α-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.

View graph of relations

© 2018 King's College London | Strand | London WC2R 2LS | England | United Kingdom | Tel +44 (0)20 7836 5454