In vitro antibacterial activities of PD 131628, a new 1,8-naphthyridine anti-infective agent.
PD 131628 is a new aminopyrrolidine-substituted fluorocyclopropyl naphthyridine quinolone which possesses high in vitro activity against a wide spectrum of bacterial species. The MICs for greater than or equal to 90% of strains were 0.125 to 0.25 microgram/ml for staphylococci, Streptococcus pyogenes, and S. pneumoniae; 0.5 micrograms/ml for S. agalactiae and Enterococcus faecalis; 0.125 micrograms/ml for members of the family Enterobacteriaceae and Acinetobacter spp.; 0.5 micrograms/ml for Pseudomonas aeruginosa; and less than or equal to 0.03 micrograms/ml for Haemophilus influenzae, Moraxella (Branhamella) catarrhalis, and Neisseria gonorrhoeae. In these in vitro comparisons with ciprofloxacin, PD 131628 is more active against gram-positive organisms, approximately equivalent against gram-negative organisms, and, like most other quinolones, relatively inactive against gram-negative anaerobes. In most instances, the in vitro potency of PD 131628 exceeded those of widely used compounds: ciprofloxacin, imipenem, ampicillin, penicillin G, oxacillin, cefazolin, ceftazidime, cefoxitin, cefsulodin, aztreonam, piperacillin, amikacin, spectinomycin, doxycycline, erythromycin, metronidazole, and vancomycin.
Cohen
M A
MA
Department of Experimental Therapy, Parke-Davis Pharmaceutical Research Division, Ann Arbor, Michigan 48105.
Huband
M D
MD
Mailloux
G B
GB
Yoder
S L
SL
Roland
G E
GE
Domagala
J M
JM
Heifetz
C L
CL
D000900:Anti-Bacterial Agents / Q000494:pharmacology*; D002939:Ciprofloxacin / Q000494:pharmacology; D024841:Fluoroquinolones; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D015378:Imipenem / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D009287:Naphthyridines / Q000494:pharmacology*
D000900:Anti-Bacterial Agents; D024841:Fluoroquinolones; D009287:Naphthyridines; C068217:PD 131628; D002939:Ciprofloxacin; D015378:Imipenem