Author/Authors :
Colin J. Dunsmore، نويسنده , , Keith Miller، نويسنده , , Katy L. Blake، نويسنده , , Simon G. Patching، نويسنده , , Peter J.F. Henderson، نويسنده , , James A. Garnett، نويسنده , , William J. Stubbings، نويسنده , , Simon E.V. Phillips، نويسنده , , Deborah J. Palestrant، نويسنده , , Joseph De Los Angeles، نويسنده , , Jennifer A. Leeds، نويسنده , , Ian Chopra، نويسنده , , Colin W.G. Fishwick، نويسنده ,
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.
Keywords :
2-Aminotetralone , MurZ inhibitor , MurA inhibitor , Antibacterial activity
