title: In vitro activity of RU 29246, the active compound of the cephalosporin prodrug ester HR 916.
abstract: The in vitro activity of RU 29246 was compared with those of other agents against 536 recent clinical isolates. The MICs of RU 29246 for 90% of members of the family Enterobacteriaceae tested (MIC90s) were less than 2 micrograms/ml except those for Morganella spp. (16 micrograms/ml) and Proteus spp. (8 micrograms/ml). RU 29246 was active against Staphylococcus aureus (MIC90, < or = 8 micrograms/ml) and against Staphylococcus saprophyticus and coagulase-negative staphylococci (MIC90s, < or = 2 micrograms/ml). Streptococci and Neisseria gonorrhoeae were highly susceptible to RU 29246, and the activity of the agent against isolates of Streptococcus pneumoniae (MIC90, < or = 0.5 micrograms/ml), Haemophilus influenzae (MIC90, < or = 2 micrograms/ml), and Moraxella catarrhalis (MIC90, < or = 2 micrograms/ml) was comparable to those of the other cephalosporins tested. RU 29246 was insusceptible to hydrolysis by the common plasmid-mediated beta-lactamases (TEM-1 and SHV-1). However, hydrolysis by the new extended-spectrum beta-lactamases (TEM-3, TEM-5, and TEM-9) was detected. Results of the study suggested that RU 29246 should be investigated clinically for use in the treatment of a wide range of infections.
authors: Department of Microbiology, Dudley Road Hospital, Birmingham, United Kingdom.
authors: G
authors: G
authors: Riess
authors: J
authors: J
authors: Andrews
authors: D
authors: D
authors: Thornber
authors: R
authors: R
authors: Wise
mesh_terms: D001441:Bacteroides fragilis / Q000187:drug effects; D002511:Cephalosporins / Q000378:metabolism / Q000494:pharmacology*; D004755:Enterobacteriaceae / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D009343:Neisseria / Q000187:drug effects; D011355:Prodrugs / Q000378:metabolism / Q000494:pharmacology*; D013211:Staphylococcus aureus / Q000187:drug effects; D013292:Streptococcus agalactiae / Q000187:drug effects; D013296:Streptococcus pneumoniae / Q000187:drug effects; D013297:Streptococcus pyogenes / Q000187:drug effects
chemical_list: D002511:Cephalosporins; C079366:HR 916; D011355:Prodrugs; C073743:RU 29246