L-658,310, a new injectable cephalosporin. I. In vitro antibacterial properties

J Antibiot (Tokyo). 1989 May;42(5):795-806. doi: 10.7164/antibiotics.42.795.

Abstract

The in vitro antibacterial spectrum of L-658,310, a new semisynthetic cephalosporin, was compared with ceftazidime, aztreonam and piperacillin against a wide variety of randomly selected human clinical isolates. The compound was found to be a broad spectrum bactericidal agent that was more potent than any of the comparison drugs against glucose nonfermenting bacteria. It has especially potent activity against Pseudomonas aeruginosa including multiply-resistant strains. The superior activity of L-658,310 against this group of organisms is attributed to the presence of the dihydroxy substituents on the 2-methylisoindoline moiety of the compound. L-658,310 is not cross-resistant with either imipenem, ceftazidime or piperacillin (representatives of three different classes of beta-lactam compounds) against P. aeruginosa. The lack of cross-resistance with ceftazidime extends to other glucose nonfermenters and several strains of Enterobacteriaceae as well. The compound is active against bacteria known to possess either R-plasmid- or chromosomally-mediated beta-lactamases.

Publication types

  • Comparative Study

MeSH terms

  • Aerobiosis
  • Anaerobiosis
  • Aztreonam / pharmacology
  • Bacteria / drug effects*
  • Ceftazidime / pharmacology
  • Cephalosporins / metabolism
  • Cephalosporins / pharmacology*
  • Drug Resistance, Microbial
  • Hydrolysis
  • Isoindoles
  • Microbial Sensitivity Tests
  • Molecular Structure
  • Piperacillin / pharmacology
  • Pseudomonas aeruginosa / drug effects
  • Structure-Activity Relationship
  • beta-Lactamases / metabolism

Substances

  • Cephalosporins
  • Isoindoles
  • BO 1236
  • Ceftazidime
  • beta-Lactamases
  • Aztreonam
  • Piperacillin