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Nanomolar inhibitors of Staphylococcus aureus methionyl tRNA synthetase with potent antibacterial activity against gram-positive pathogens.
- Source :
-
Journal of medicinal chemistry [J Med Chem] 2002 May 09; Vol. 45 (10), pp. 1959-62. - Publication Year :
- 2002
-
Abstract
- 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.
- Subjects :
- Abscess drug therapy
Abscess microbiology
Animals
Anti-Bacterial Agents chemistry
Anti-Bacterial Agents pharmacology
Drug Resistance, Bacterial
Enzyme Inhibitors chemistry
Enzyme Inhibitors pharmacology
Quinolones chemistry
Quinolones pharmacology
Rats
Rats, Sprague-Dawley
Staphylococcus aureus drug effects
Staphylococcus aureus enzymology
Structure-Activity Relationship
Anti-Bacterial Agents chemical synthesis
Enterococcus drug effects
Enzyme Inhibitors chemical synthesis
Methionine-tRNA Ligase antagonists & inhibitors
Quinolones chemical synthesis
Staphylococcus drug effects
Subjects
Details
- Language :
- English
- ISSN :
- 0022-2623
- Volume :
- 45
- Issue :
- 10
- Database :
- MEDLINE
- Journal :
- Journal of medicinal chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 11985462
- Full Text :
- https://doi.org/10.1021/jm025502x