Title of article
Anthranilate 4H-oxazol-5-ones: novel small molecule antibacterial acyl carrier protein synthase (AcpS) inhibitors
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 ,
Issue Information
روزنامه با شماره پیاپی سال 2004
Pages
5
From page
37
To page
41
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+.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2004
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
793920
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