In vitro activity of RU 29246, the active compound of the cephalosporin prodrug ester HR 916

Antimicrob Agents Chemother. 1992 Nov;36(11):2360-4. doi: 10.1128/AAC.36.11.2360.

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.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Bacteroides fragilis / drug effects
  • Cephalosporins / metabolism
  • Cephalosporins / pharmacology*
  • Enterobacteriaceae / drug effects
  • Microbial Sensitivity Tests
  • Neisseria / drug effects
  • Prodrugs / metabolism
  • Prodrugs / pharmacology*
  • Staphylococcus aureus / drug effects
  • Streptococcus agalactiae / drug effects
  • Streptococcus pneumoniae / drug effects
  • Streptococcus pyogenes / drug effects

Substances

  • Cephalosporins
  • HR 916
  • Prodrugs
  • RU 29246