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Nanomolar inhibitors of Staphylococcus aureus methionyl tRNA synthetase with potent antibacterial activity against gram-positive pathogens.

Authors:
Richard L Jarvest John M Berge Valerie Berry Helen F Boyd Murray J Brown John S Elder Andrew K Forrest Andrew P Fosberry Daniel R Gentry Martin J Hibbs Deborah D Jaworski Peter J O'Hanlon Andrew J Pope Stephen Rittenhouse Robert J Sheppard Courtney Slater-Radosti Angela Worby

J Med Chem 2002 May;45(10):1959-62

Potent nanomolar inhibitors of Staphylococcus aureus methionyl tRNA synthetase have been derived from a file compound high throughput screening hit. Optimized compounds show excellent antibacterial activity against staphylococcal and enterococcal pathogens, including strains resistant to clinical antibiotics. Compound 11 demonstrated in vivo efficacy in an S. aureus rat abscess infection model.

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http://dx.doi.org/10.1021/jm025502xDOI Listing
May 2002

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