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
Rok vydání: 1995
Předmět:
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