Synthesis and antibacterial properties of β-diketone acrylate bioisosteres of pseudomonic acid A
| Autor: | Nigel J. P. Broom, John Stephen Elder, Nicky D. Masson, Isobel Bennett, Robert Cassels, Peter J. O'Hanlon |
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| Rok vydání: | 1999 |
| Předmět: |
Male
Staphylococcus aureus Clinical Biochemistry Pharmaceutical Science Epoxide Biochemistry Chemical synthesis Mice chemistry.chemical_compound Drug Discovery Animals Organic chemistry Molecular Biology Antibacterial agent Diketone Acrylate biology Organic Chemistry Ketones Anti-Bacterial Agents Kinetics Mupirocin chemistry Enzyme inhibitor biology.protein Molecular Medicine Bioisostere Antibacterial activity |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 9:1847-1852 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/s0960-894x(99)00296-6 |
| Popis: | A series of beta-diketone acrylate bioisosteres 4 of pseudomonic acid A 1 have been synthesized and evaluated for their ability to inhibit bacterial isoleucyl-tRNA synthetase and act as antibacterial agents. A number of analogues have excellent antibacterial activity. Selected examples were shown to afford good blood levels and to be effective in a murine infection model. |
| Databáze: | OpenAIRE |
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