In Vitro and in Vivo Activities of Clinafloxacin, CI-990 (PD 131112), and PD 138312 Versus Enterococci
Overview
Affiliations
Certain new fluoroquinolones have high activity against enterococci. Against Enterococcus faecalis (n = 18), MICs at which 90% of the isolates were inhibited were as follows (in micrograms per milliliter): clinafloxacin, 0.125; CI-990, 0.5; and PD 138312, 0.25 (compared with 1 microgram/ml for ciprofloxacin and 2 micrograms/ml for ofloxacin). Strains producing beta-lactamase or that were vancomycin resistant or resistant to high-level gentamicin were not quinolone cross-resistant. The drugs were bactericidal and were unaffected by 50% human serum. Oral efficacies (in milligrams per kilogram of body weight for 50% protective doses) in lethal mouse infections with quinolone-susceptible strains were 4.3 to 24 for clinafloxacin, 7.2 to 39 for CI-990, 7.2 to 76 for PD 138312, and 41 to > 100 for ciprofloxacin; when the drugs were given subcutaneously, the order was similar and values ranged from 1.1 to 12.5. Clinafloxacin, CI-990, and PD 138312 may have therapeutic potential in systemic enterococcal infections in humans.
Antimicrobial Activity of Naphthyridine Derivatives.
Wojcicka A, Maczynski M Pharmaceuticals (Basel). 2025; 17(12.
PMID: 39770547 PMC: 11678664. DOI: 10.3390/ph17121705.
Eradication of Biofilm Infection by Persister Drug Combination.
Yee R, Yuan Y, Tarff A, Brayton C, Gour N, Feng J Antibiotics (Basel). 2022; 11(10).
PMID: 36289936 PMC: 9598165. DOI: 10.3390/antibiotics11101278.
Huband M, Cohen M, Zurack M, Hanna D, Skerlos L, Sulavik M Antimicrob Agents Chemother. 2007; 51(4):1191-201.
PMID: 17261623 PMC: 1855495. DOI: 10.1128/AAC.01321-06.
Intravenous mouse infection model for studying the pathology of Enterococcus faecalis infections.
Gentry-Weeks C, Estay M, Loui C, Baker D Infect Immun. 2003; 71(3):1434-41.
PMID: 12595461 PMC: 148842. DOI: 10.1128/IAI.71.3.1434-1441.2003.
Clark C, Jacobs M, Appelbaum P Antimicrob Agents Chemother. 1999; 43(9):2295-8.
PMID: 10471582 PMC: 89464. DOI: 10.1128/AAC.43.9.2295.