title: L-658,310, a new injectable cephalosporin. I. In vitro antibacterial properties.
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.
authors.affiliation: Merck Sharp & Dohme Research Laboratories, Rahway, New Jersey 07065-0900.
authors.forename: B A
authors.initials: BA
authors.lastname: Weissberger
authors.forename: G K
authors.initials: GK
authors.lastname: Abruzzo
authors.forename: R A
authors.initials: RA
authors.lastname: Fromtling
authors.forename: C
authors.initials: C
authors.lastname: Gill
authors.forename: S
authors.initials: S
authors.lastname: Ponticas
authors.forename: M E
authors.initials: ME
authors.lastname: Valiant
authors.forename: D L
authors.initials: DL
authors.lastname: Shungu
authors.forename: H H
authors.initials: HH
authors.lastname: Gadebusch
mesh_terms: D000332:Aerobiosis; D000693:Anaerobiosis; D001398:Aztreonam / Q000494:pharmacology; D001419:Bacteria / Q000187:drug effects*; D002442:Ceftazidime / Q000494:pharmacology; D002511:Cephalosporins / Q000378:metabolism / Q000494:pharmacology*; D004352:Drug Resistance, Microbial; D006868:Hydrolysis; D054833:Isoindoles; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D010878:Piperacillin / Q000494:pharmacology; D011550:Pseudomonas aeruginosa / Q000187:drug effects; D013329:Structure-Activity Relationship; D001618:beta-Lactamases / Q000378:metabolism
chemical_list: D002511:Cephalosporins; D054833:Isoindoles; C053266:BO 1236; D002442:Ceftazidime; D001618:beta-Lactamases; D001398:Aztreonam; D010878:Piperacillin