Cinoxacin: Effectiveness Against Experimental Pyelonephritis in Rats

Holmes, D. H.; Ensminger, P. W.; Gordee, Robert S.

doi:10.1128/aac.6.4.432

Cited by 15 publications

(7 citation statements)

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“…Cinoxacin belongs to the same class of antimicrobial drugs as nalidixic acid and oxolinic acid which are used in the treatment of urinary tract infections. Its antibacterial activity is similar to these drugs in vitro and perhaps superior in vivo against experimental pyelonephritis in rats (1,5 Research Institute. Stock solutions of 2,000 Ag of each drug per ml were prepared in phosphate buffer (pH 7), stored at -20 C, and used within 6 weeks.…”

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confidence: 77%

“…Cinoxacin belongs to the same class of antimicrobial drugs as nalidixic acid and oxolinic acid which are used in the treatment of urinary tract infections. Its antibacterial activity is similar to these drugs in vitro and perhaps superior in vivo against experimental pyelonephritis in rats (1,5). In this study a series of observations were made to further evaluate the antimicrobial action of cinoxacin against recent clinical isolates and compare its activity with nalidixic acid.…”

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confidence: 99%

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Antibacterial Activity of Cinoxacin In Vitro

Giamarellou

Jackson

1975

Antimicrob Agents Chemother

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Cinoxacin is a new synthetic compound similar chemically and in antimicrobial activity to oxolonic acid and nalidixic acid. It is most effective against Escherichia coli and Proteus mirabilis, but at concentrations expected in the urine it is inhibitory for all species of Enterobacteriaceae. Relative to nalidixic acid, cinoxacin has slightly greater inhibitory and bactericidal activity, less inoculum effect probably due to less heterogeneity in the susceptibility of bacterial cells, and less inhibition by high concentrations of serum protein. Both drugs are more active in an acid than an alkaline medium. Glucose can specifically antagonize the inhibitory effect against P. mirabilis. In urine the bactericidal rate and effect are decreased. Resistance to cinoxacin can be developed quickly by serial.transfers in vitro. Some nonresistant organisms remained viable in bactericidal drug concentrations. The in vivo importance of the favorable features of cinoxacin must be determined by clinical trials.Cinoxacin is a new synthetic compound with antibacterial activity (5). The name is derived from the basic ring structure which is a cinnoline (1-2 benzodiozine). Chemically, the compound is 1-ethyl-1,4-dihydro-4-oxo-(1,3)-dioxolo-(4,5-g)cinnoline-3-carboxylic acid. Cinoxacin belongs to the same class of antimicrobial drugs as nalidixic acid and oxolinic acid which are used in the treatment of urinary tract infections. Its antibacterial activity is similar to these drugs in vitro and perhaps superior in vivo against experimental pyelonephritis in rats (1,5 Research Institute. Stock solutions of 2,000 Ag of each drug per ml were prepared in phosphate buffer (pH 7), stored at -20 C, and used within 6 weeks. Minimal inhibitory concentrations (MIC) for cinoxacin and nalidixic acid were determined by the standard tube dilution or microtiter technique. The basic medium was tryptose phosphate broth which was modified for specific tests by adjustment of pH, or by the addition of defined amounts of horse serum, sodium chloride, sucrose, dextrose, or urea. Urine that was used as a bacteriologic medium was obtained from healthy adults, pooled, and filtered through a sterilizing filter. Serial twofold dilutions of drug standards were made in tryptose phosphate broth, yielding drug concentrations from 500 to 0.25 gg/ml. The standard bacterial inoculum was a 1:1,000 dilution of a log-phase bacterial culture, yielding a final concentration of approximately 106 bacteria per ml. The MIC end point was determined by visual turbidity after 16 to 18 h of incubation at 37 C. Most of the strains tested by the broth dilution methods were retested by the agar disk diffusion method using 30 ,ig disks of each drug.The minimal bactericidal concentration (MBC) was determined from the clear tubes in the sensitivity test by quantitative subculture onto semisolid media. The MBC end point was designated as that concentration of antibiotic that produced a reduction in viable organisms of at least 4 logs or 99.99%. Bactericidal rates were determined by count...

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confidence: 77%

“…Cinoxacin belongs to the same class of antimicrobial drugs as nalidixic acid and oxolinic acid which are used in the treatment of urinary tract infections. Its antibacterial activity is similar to these drugs in vitro and perhaps superior in vivo against experimental pyelonephritis in rats (1,5). In this study a series of observations were made to further evaluate the antimicrobial action of cinoxacin against recent clinical isolates and compare its activity with nalidixic acid.…”

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confidence: 99%

Antibacterial Activity of Cinoxacin In Vitro

Giamarellou

Jackson

1975

Antimicrob Agents Chemother

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“…The six organism species tested represent six of the a Includes Pseudomonas maltophilia (6), P. stutzeri (3), P. cepacia (2), and Pseudomonas species (2). b Includes Pasteurella multocida (4), Aeromonas hydrophilia (3), enteropathogenic E. coli (3), Shigella species (22), Salmonella enteritidis (7), and one strain each ofEF4, Ve type 2, Vd, 11K type 1, Achromobacter xylosoxidans, Flavobacterium species, and gram-negative bacillus NOS.…”

Section: Resultsmentioning

confidence: 99%

“…The activity of cinoxacin was slightly greater than that of nalidixic acid.A number of synthetic organic acids containing cinnoline ring structures have been investigated for antimicrobial activity (3,8). Of these compounds, cinoxacin (1-ethyl-1,4-dihydro-4,oxo-[1,3] Susceptibility testing.…”

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In Vitro Antimicrobial Activity of Cinoxacin Against 2,968 Clinical Bacterial Isolates

Jones

Fuchs²

1976

Antimicrob Agents Chemother

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Cinoxacin demonstrated effective in vitro antimicrobial activity against the Enterobacteriaceae, but negligible activity against Pseudomonas aeruginosa and gram-positive cocci. The activity of cinoxacin was slightly greater than that of nalidixic acid.A number of synthetic organic acids containing cinnoline ring structures have been investigated for antimicrobial activity (3,8). Of these compounds, cinoxacin (1-ethyl-1,4-dihydro-4,oxo-[1,3] Susceptibility testing. MICs of all antimicrobial agents were determined by the broth microdilution technique. Mueller-Hinton broth (Difco) was used in previously prepared well plastic trays (8 by 10; Micro-Media Systems, Inc., Campbell, Calif.). The antimicrobial agents were injected into the wells in 100-Al volumes. Organisms were grown to stationary phase (109 organisms/ml) in brain heart infusion broth and then diluted 1:100 in sterile water. An automatic tray inoculator delivered 5 Al of this dilution to each 100-,ul well; final inoculum concentration was 5 x 10'5 organisms/ml.In the inoculum size studies, organisms were inoculated as above, using similar equipment and three inoculum concentrations, 107, 10', and 103 organisms/ml. MIC end points were defined as the lowest broth concentration totally inhibiting organism growth (clear well) after 15 to 18 h of incubation at 35 C. Determination of the MBC was performed by subculturing 1 MAl of both turbid and clear wells into Mueller-Hinton broth. The MBC was defined as the lowest subcultured broth concentration revealing no growth (clear well) after overnight incubation at 35 C. This represents a three-log minimum-kill (99.9%) end point. RESULTS AND DISCUSSIONThe cumulative percentage of gram-negative bacilli inhibited by increasing cinoxacin concentrations is shown in Table 1. Among the 2,139 strains tested, Escherichia coli, Citrobacter diversus, Proteus morganii, and Proteus vulgaris exhibited the greatest susceptibility. Ten of the thirteen tabulated Enterobacteriaceae species showed greater than 90% inhibition of strains at 16 ,ug/ml. Only Proteus mirabilis, Proteus rettgeri, and Providencia species demonstrated a relative resistance to cinoxacin. All P. morganii and P. vulgaris strains were inhibited by 4 ug/ml in contrast to 67 and 0% for Proteus rettgeri and Providencia species, respectively. Only 12 of 210 pseudomonas isolates had MIC values of 64 jig/ml or less. However, 43 of the 57 non-Enterobacteriaceae, nonpseudomonas gram-negative isolates had MIC values of 64 Ag/ml or less.The data in Table 2 confirm the poor cinoxacin antimicrobial activity against gram-positive organisms. Of note, however, was the 26 to 28% inhibitory response of staphylococcus isolates. Only 2 of 191 streptococcus strains had MIC values of 64 ,ug/ml or less.The comparison of cinoxacin and nalidixic acid MICs and MBCs is shown in Table 3. The six organism species tested represent six of the

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Development of antibacterial agents of the nalidixic acid type

Albrecht¹

1977

Progress in Drug Research / Fortschritte Der Arzneimittelforschung / Progrès Des Rechersches Pharmaceutiques

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Cinoxacin: Effectiveness Against Experimental Pyelonephritis in Rats

Cited by 15 publications

References 4 publications

Antibacterial Activity of Cinoxacin In Vitro

Antibacterial Activity of Cinoxacin In Vitro

In Vitro Antimicrobial Activity of Cinoxacin Against 2,968 Clinical Bacterial Isolates

Development of antibacterial agents of the nalidixic acid type

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