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ID: ALA1141516

Journal: Bioorg Med Chem Lett

Title: 2-Aminotetralones: novel inhibitors of MurA and MurZ.

Authors: Dunsmore CJ, Miller K, Blake KL, Patching SG, Henderson PJ, Garnett JA, Stubbings WJ, Phillips SE, Palestrant DJ, Angeles Jde L, Leeds JA, Chopra I, Fishwick CW.

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.

CiteXplore: 18261901

DOI: 10.1016/j.bmcl.2008.01.089