Abstract
DuP 721 (p-acetylphenyloxooxazolidinylmethylacetamide) and DuP 105 (a methylsulfinyl derivative) are orally active representatives of the oxazolidinones, a new class of synthetic antibacterial agents. Their antibacterial spectrum includes staphylococci, streptococci, and Bacteroides fragilis strains. The compounds have equal activity against staphylococcal strains susceptible or resistant to beta-lactam antibiotics, including methicillin-resistant strains. The MICs for 90% of the strains (MIC90s) against staphylococcal isolates were 1 to 4 micrograms/ml for DuP 721 and 4 to 16 micrograms/ml for DuP 105, compared with 1 to 2 micrograms/ml for vancomycin, 0.5 microgram/ml for ciprofloxacin, and 2 to greater than 16 micrograms/ml for imipenem. The MIC90s against group D streptococci were 4 micrograms/ml for DuP 721, 16 micrograms/ml for DuP 105, and 2 micrograms/ml for vancomycin, ciprofloxacin, and imipenem. MIC90s against B. fragilis isolates were 4 micrograms/ml for DuP 721, 16 micrograms/ml for DuP 105, and 8 micrograms/ml for cefoxitin. DuP 721 and DuP 105 administered by either the oral or the parenteral route were protective against staphylococcal and streptococcal infections in mice. The 50% effective doses were 2 to 10 mg/kg for DuP 721, 9 to 23 mg/kg for DuP 105, and 2 to 12 mg/kg for vancomycin. These results indicate that further studies of compounds of the oxazolidinone series are warranted.
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Selected References
These references are in PubMed. This may not be the complete list of references from this article.
- Grappel S. F., Phillips L., Lewis H. B., Morgan D. G., Actor P. Prophylactic activity of cephalosporins in a mouse model of surgical wound infection. J Antibiot (Tokyo) 1983 Feb;36(2):161–166. doi: 10.7164/antibiotics.36.161. [DOI] [PubMed] [Google Scholar]
- Haley R. W., Hightower A. W., Khabbaz R. F., Thornsberry C., Martone W. J., Allen J. R., Hughes J. M. The emergence of methicillin-resistant Staphylococcus aureus infections in United States hospitals. Possible role of the house staff-patient transfer circuit. Ann Intern Med. 1982 Sep;97(3):297–308. doi: 10.7326/0003-4819-97-3-297. [DOI] [PubMed] [Google Scholar]
- Lowy F. D., Hammer S. M. Staphylococcus epidermidis infections. Ann Intern Med. 1983 Dec;99(6):834–839. doi: 10.7326/0003-4819-99-6-834. [DOI] [PubMed] [Google Scholar]
- Saravolatz L. D., Markowitz N., Arking L., Pohlod D., Fisher E. Methicillin-resistant Staphylococcus aureus. Epidemiologic observations during a community-acquired outbreak. Ann Intern Med. 1982 Jan;96(1):11–16. doi: 10.7326/0003-4819-96-1-11. [DOI] [PubMed] [Google Scholar]
- Schwalbe R. S., Stapleton J. T., Gilligan P. H. Emergence of vancomycin resistance in coagulase-negative staphylococci. N Engl J Med. 1987 Apr 9;316(15):927–931. doi: 10.1056/NEJM198704093161507. [DOI] [PubMed] [Google Scholar]
- Tenney J. H., Maack R. W., Chippendale G. R. Rapid selection of organisms with increasing resistance on subinhibitory concentrations of norfloxacin in agar. Antimicrob Agents Chemother. 1983 Jan;23(1):188–189. doi: 10.1128/aac.23.1.188. [DOI] [PMC free article] [PubMed] [Google Scholar]