Anthranilate 4H-oxazol-5-ones: novel small molecule antibacterial acyl carrier protein synthase (AcpS) inhibitors |
| |
| Authors: | Gilbert Adam M Kirisits Matthew Toy Patrick Nunn David S Failli Amadeo Dushin Elizabeth G Novikova Elena Petersen Peter J Joseph-McCarthy Diane McFadyen Iain Fritz Christian C |
| |
| Institution: | Department of Chemical and Screening Sciences, Wyeth Research, 401N. Middletown Road, Pearl River, NY 10945, USA. gilbera@wyeth.com |
| |
| Abstract: | D-optimal design and Projection to Latent Structures (PLS) analysis were used to optimize screening hit 5 (B. subtilis AcpS IC(50): 15 microM, B. subtilis MIC: >200 microM) into a series of 4H-oxazol-5-one, small molecule, antibacterial, AcpS inhibitors. Specifically, 15, 16 and 18 show microM or sub-microM AcpS inhibition (IC(50)s: 15: 1.1 microM, 16: 1.5 microM, 18: 0.27 microM) and moderate antibacterial activity (MICs: 12.5-50 microM) against B. subtilis, E. faecalis ATCC, E. faecalis VRE and S. pneumo+. |
| |
| Keywords: | |
| 本文献已被 PubMed 等数据库收录！ |
|
