Author/Authors :
Adam M. Gilbert، نويسنده , , Matthew Kirisits، نويسنده , , Patrick Toy، نويسنده , , David S. Nunn، نويسنده , , Amadeo Failli، نويسنده , , Elizabeth G. Dushin، نويسنده , , Elena Novikova، نويسنده , , Peter J. Petersen، نويسنده , , Diane Joseph-McCarthy، نويسنده , , Iain McFadyen، نويسنده , , Christian C. Fritz and Robert Powers، نويسنده ,
Abstract :
D-optimal design and Projection to Latent Structures (PLS) analysis were used to optimize screening hit 5 (B. subtilis AcpS IC50: 15 μM, B. subtilis MIC: >200 μM) into a series of 4H-oxazol-5-one, small molecule, antibacterial, AcpS inhibitors. Specifically, 15, 16 and 18 show μM or sub-μM AcpS inhibition (IC50s: 15: 1.1 μM, 16: 1.5 μM, 18: 0.27 μM) and moderate antibacterial activity (MICs: 12.5–50 μM) against B. subtilis, E. faecalis ATCC, E. faecalis VRE and S. pneumo+.
