SB 205952, a novel semisynthetic monic acid analog with at least two modes of action
Autor: | R Cassels, Ian Chopra, Peter J. O'Hanlon, Brunello Oliva, J M Wilson |
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Rok vydání: | 1995 |
Předmět: |
DNA
Bacterial Staphylococcus aureus Stringent response Stereochemistry Mupirocin Microbial Sensitivity Tests chemistry.chemical_compound Bacterial Proteins Escherichia coli medicine Pharmacology (medical) Oxazoles Antibacterial agent Pharmacology chemistry.chemical_classification Bacteria biology RNA Anti-Bacterial Agents RNA Bacterial Infectious Diseases Enzyme chemistry Biochemistry Mechanism of action Enzyme inhibitor biology.protein lipids (amino acids peptides and proteins) medicine.symptom DNA Research Article |
Zdroj: | Antimicrobial Agents and Chemotherapy. 39:1925-1933 |
ISSN: | 1098-6596 0066-4804 |
DOI: | 10.1128/aac.39.9.1925 |
Popis: | The biological properties of SB 205952, a nitrofuryl oxazole derivative of monic acid, differ from those of the closely related antibacterial agent mupirocin. Compared with mupirocin, SB 205952 has increased antimicrobial potency, an extended spectrum including mupirocin-resistant staphylococci, and rapid bactericidal activity. SB 205952, like mupirocin, is a potent inhibitor of bacterial isoleucyl-tRNA synthetase (IRS) in mupirocin-susceptible organisms but does not inhibit IRS from mupirocin-resistant staphylococci, indicating that SB 205952 has more than one mechanism of action. SB 205952 rapidly inhibits protein, RNA, and DNA syntheses in mupirocin-susceptible and mupirocin-resistant staphylococci. In each case, the effect on RNA synthesis is relaxed by treatment with chloramphenicol, indicating that inhibition of RNA synthesis is probably a secondary consequence of stringent control. It is proposed that SB 205952 possesses one or more mechanisms of action in addition to IRS inhibition, probably mediated by its nitrofuryl component. |
Databáze: | OpenAIRE |
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