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Conformational restriction of methionyl tRNA synthetase inhibitors leading to analogues with potent inhibition and excellent gram-positive antibacterial activity
- Source :
- Bioorganicmedicinal chemistry letters. 13(7)
- Publication Year :
- 2003
-
Abstract
- Conformationally restricted analogues of the central linker unit of bacterial methionyl tRNA synthetase (MRS) inhibitors have been prepared. The (1S,2R)-cyclopentylmethyl moiety was identified as the preferred cyclic linker, with significant diastereo- and enantioselectivity of activity. Combination of this linker with an optimal substituted aryl right-hand side has resulted in a compound with exceptionally good antibacterial activity against staphylococci and enterococci, including antibiotic resistant strains.
- Subjects :
- Models, Molecular
Staphylococcus aureus
Methionine—tRNA ligase
Stereochemistry
Protein Conformation
Clinical Biochemistry
Pharmaceutical Science
Methionine-tRNA Ligase
In Vitro Techniques
Gram-Positive Bacteria
Biochemistry
Chemical synthesis
Drug Discovery
Enterococcus faecalis
Moiety
Animals
Enzyme Inhibitors
Molecular Biology
Antibacterial agent
chemistry.chemical_classification
biology
Chemistry
Organic Chemistry
Stereoisomerism
Anti-Bacterial Agents
Rats
Enzyme
Liver
Enzyme inhibitor
biology.protein
Molecular Medicine
Indicators and Reagents
Antibacterial activity
Linker
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 13
- Issue :
- 7
- Database :
- OpenAIRE
- Journal :
- Bioorganicmedicinal chemistry letters
- Accession number :
- edsair.doi.dedup.....0c6b1acdbb35559eeda1b6cb7a1637e4