Antibacterial oxazolidinones. In vitro activity of a new analogue, E3709.
The oxazolidinone compound E3709, which contains a 4-pyridyl group, was found to be more active in vitro than other members of this series, such as DuP 721. MIC90 for staphylococci(including methicillin-resistant isolates), streptococci (including Enterococcus faecalis), Clostridia, and diphtheroids was less than 0.5 micrograms/ml. Haemophilus influenzae, Moraxella catarrhalis, and Bacteroides fragilis were less susceptible, with an MIC90 between 2 and 8 micrograms/ml. E3709 MICs of Gram-negative species ranged from 100 to greater than 1000 micrograms/ml. At a concentration of 10 micrograms/ml, E3709 was bactericidal for selected Gram-positive species. A postantibiotic effect of 3 hr was observed against staphylococci. Resistance to E3709 was not detected.
Brumfitt
W
W
Department of Medical Microbiology, Royal Free Hospital School of Medicine, London, UK.
Hamilton-Miller
J M
JM
D000667:Ampicillin / Q000494:pharmacology; D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology*; D002433:Cefaclor / Q000494:pharmacology; D006094:Gram-Positive Bacteria / Q000187:drug effects* / Q000254:growth & development; D008826:Microbial Sensitivity Tests; D010080:Oxazoles / Q000494:pharmacology; D023303:Oxazolidinones; D011725:Pyridines / Q000737:chemistry / Q000494:pharmacology*; D013752:Tetracycline / Q000494:pharmacology; D013997:Time Factors; D014640:Vancomycin / Q000494:pharmacology
D000900:Anti-Bacterial Agents; D010080:Oxazoles; D023303:Oxazolidinones; D011725:Pyridines; C054755:4-acetylphenyloxooxazolidinylmethylacetamide; C078263:E 3709; D002433:Cefaclor; D014640:Vancomycin; D000667:Ampicillin; D013752:Tetracycline