» Articles » PMID: 8540728

In Vitro and in Vivo Activities of Clinafloxacin, CI-990 (PD 131112), and PD 138312 Versus Enterococci

Overview
Specialty Pharmacology
Date 1995 Sep 1
PMID 8540728
Citations 12
Authors
Affiliations
Soon will be listed here.
Abstract

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.

Citing Articles

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.


In vitro and in vivo activities of PD 0305970 and PD 0326448, new bacterial gyrase/topoisomerase inhibitors with potent antibacterial activities versus multidrug-resistant gram-positive and fastidious organism groups.

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.


Activities of clinafloxacin, alone and in combination with other compounds, against 45 gram-positive and -negative organisms for which clinafloxacin MICs are high.

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.


References
1.
KIRBY W, Regamey C . Pharmacokinetics of cefazolin compared with four other cephalosporins. J Infect Dis. 1973; 128:Suppl:S341-6. DOI: 10.1093/infdis/128.supplement_2.s341. View

2.
Shlaes D, Rice L . Bacterial resistance to the cyclic glycopeptides. Trends Microbiol. 1994; 2(10):385-8. DOI: 10.1016/0966-842x(94)90616-5. View

3.
Fuchs P, Barry A, Pfaller M, Allen S, Gerlach E . Multicenter evaluation of the in vitro activities of three new quinolones, sparfloxacin, CI-960, and PD 131,628, compared with the activity of ciprofloxacin against 5,252 clinical bacterial isolates. Antimicrob Agents Chemother. 1991; 35(4):764-6. PMC: 245095. DOI: 10.1128/AAC.35.4.764. View

4.
Cohen M, Huband M, Mailloux G, Yoder S, Roland G, Heifetz C . In vitro antibacterial activities of the fluoroquinolones PD 117596, PD 124816, and PD 127391. Diagn Microbiol Infect Dis. 1991; 14(3):245-58. DOI: 10.1016/0732-8893(91)90039-i. View

5.
Moellering Jr R . The Garrod Lecture. The enterococcus: a classic example of the impact of antimicrobial resistance on therapeutic options. J Antimicrob Chemother. 1991; 28(1):1-12. DOI: 10.1093/jac/28.1.1. View