• YAKHAK HOEJI
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• v.47 no.6
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• pp.365-368
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• 2003

The bactericidal activities of DW286, a new fluoroquinolone were investigated by comparing the minimal bactericidal concentrations (MBCs) and the time-kill curve of it against some Gram-positive and Gram-negative bacterial strains. The MBCs of DW286 for the strains tested were either equal to or two-fold higher than the MICs, as were observed for the other fluoroquinolones. And DW286 exhibited rapid killing curves against the strains. Accordingly, it could be said that DW286 has bactericidal activity comparable to other fluoroquinolones.

• YAKHAK HOEJI
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• v.40 no.3
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• pp.343-346
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• 1996

The influence of LB20304a, a new fluoroquinolone antibiotic agent, on microflora of caecum in mice was compared with those of ciprofloxacin and piperacillin after administration of drugs for 5 days. Selective medium (CCFMA) was used for the isolation of Clostridium difficile from the specimens of mouse caecum. The emergence of C. difficile in mouse caecum induced by LB20304a was lower than that by ciprofloxacin or piperacillin at day 1 and day 7 after completing administration of drugs.

• YAKHAK HOEJI
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• v.31 no.2
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• pp.98-104
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• 1987

The compounds synthesized by authors were evaluated for their antimicrobial activities against. Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Proteus vulgaris and Pseudomonas aeraginosa New compounds[1, 10] possess striking potency against a wide range of microorganisms, especially the Gram negative aerobes and has spectacular activity against Enterobacteriaces, S. aureus and Ps. aeruginosa. Most of new compounds are very active in vitro against most strains of Enter- bacteriaceae and Gram positive aerobes, but moderately active against Ps. aeruginosa.

• YAKHAK HOEJI
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• v.43 no.1
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• pp.131-133
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• 1999

The bactericidal activities of DW-116, a new fluoroquinolone was estimated by comparing the minimal bactericidal concentrations (MBCs) of it against some Gram-positive and -negative bacterial strains with the minimal inhibitory concentrations (MICs). The MBCs against the test organisms were equal to or two times higher than MICs. The results support that the antibacterial activity of DW-116 is bactericidal.

• The Journal of the Korean Society for Microbiology
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• v.35 no.5_6
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• pp.337-339
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• 2000

MRSA, erythromycin-resistant S. pyogenes, penicillin non-susceptible pneumococci, PPNG, ESBL-producing E. coli and K. pneumoniae, class C ${\beta}$-lactamase-producing E. coli, fluoroquinolone-resistant E. coli, aminoglycoside-resistant A. baumannii and P. aeruginosa are all prevalent in Korea, which suggest the presence of high levels of antimicrobial selective pressure and nosocomial spread of resistant bacteria. Rapid increase of VRE and emergence of fluoroquinolone-resistant gonococci and VIM-2 metallo-${\beta}$-lactamase-producing P. aeruginosa are recently observed new threats in Korea.

• Archives of Pharmacal Research
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• v.19 no.4
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• pp.317-320
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• 1996

The time-kill curves of LB20304, a novel fluoroquinolone that has potent antibacterial activity against gram-positve and gram-negative bacteria, were calculated at the concentrations of 1/4-, 1/2-, 1-, 2- and 4-times the MIC against Staphylococcus aureus 77, Escherichia coli 3739E, Pseudomonas aeruginosa 1912E. The bactericidal activity of LB20304 for these strains was very rapid and comparable to that of ciprofloxacin. LB20304 produced a decrease in the $log_10$ CFU per milliliter of${\geq}$3 within 2 h at 4-times the MIC for all strains and consitently prevented regrowth of bacteria after 24 h of incubation. The MBCs (Minimal Bactericidal Concentration) of LB20304 against test organisms were equal to or at most four-times higher than the MICs.

• Archives of Pharmacal Research
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• v.20 no.4
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• pp.358-362
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• 1997

Metabolite identification and urinary and biliary excretion of the new fluoroquinolone antibacterial agent DW116 [1-(5-fluoro-2-pyridyl)-6-fluoro-7-(4-methyl-1 -piperazinyl)-1, 4-dihydro-4-oxoquinoline-3-carboxylic acid, hydrochloride] after oral administration have been studied in Sprague-Dawley rats. The excretion kinetics were monoexponential. Most of the drug was eliminated via the hepatic and renal routes. Mean renal clearance of DW116 was 73.4 ml/hr/kg and mean biliary clearance was 83.8 ml/hr/kg. The major metabolite excreted in the bile was identified as the glucuronide ester of the parent drug using base-hydrolysis of the conjugate metabolite followed by co-HPLC with standard compound, $^{19}$ F-NMR and LC-MS methods. The glucuronide conjugate was also found in urine. The mean urinary recoveries of free and total (free plus glucuronide ester) DW116 were $28.6{\pm}2.7% $and $36.4{\pm}1.8%$ of the administered dose and the corresponding biliary recoveries were $14.4{\pm} 5.5%$ and $37.0{\pm}7.6%$, respectively.

• Archives of Pharmacal Research
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• v.16 no.1
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• pp.6-12
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• 1993

To evaluate KR-10876, a new fluoroquinolone antibacterial agent, its effects on the central nervous system(CNS) were investigated in mmice as part of phamacological study, and the results were compared with those for ciprofloxacin and ofloxacin, two prototypes of quinolone antiabctrial agents. All the parameters indicative of CNS function and acute toxicity were measured by close observation of the animals at regular time intervals after oral treatment of test compounds. KR-10876 did not have any effect on the parameters measured at lower does (100, 300 mg/kg, p.o.), it caused ptosis, suppressed spontaneous locomotor activity, hypothemia, and prolonged hexobarbital-induced sleeping time. KR-10876 also had a slight effect on motor coordination only at high dose. Simialr to ciprofloxacin, KR-10876 did not protect mice from pentylenetetrazol-strychnine-, and electroshock-inducedl convulsions at doses tested. These findings demonstrate that KR-10876 affects CNS functions only at high doses. The rank order for effects is ofloxacin$\le$KR-10876>ciprofloxacin.

• Archives of Pharmacal Research
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• v.19 no.5
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• pp.400-405
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• 1996

In vitro studies were conducted to dertermine the frequency rate of spontaneous resistance to LB20304 and to dertermine whether cross-resistance to other antimicrobial agents develops. In eight strains of bacteria, the frequency of mutation to LB20304 at the concentrations of four and eight times the minimal inhibitory concentration(MIC) ranaged from less than 4.0 ${\times}$ $10^{-10}$ to 2.2 $\{times}$ $10^{-10}$ . These results were similar to those founf for other new fluoroquinolones. THe development of stepwise resistance was determined by repeated subculture in broth in the presence of increasing concentration of the compounds. Exposure of bacteria to increasing concentrations of LB20304 resulted in the selection of organisms with higher MICs. There were 4- to 128-fold increases in the MIC of LB20304 for bacterial strains of Staphylococcus aureus, Streptococcus pneumoniae, Escherichia coli and Pseudomonas aeruginosa. However, those strains selected after repeated exposure were well within the susceptibility range for LB20304 except for Pseudomonas aeruginosa. The resistant isolates selected with LB20304 showed cross-resistance when tested against ciprofloxacin and vice versa.

• Biomolecules & Therapeutics
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• v.6 no.2
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• pp.165-170
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• 1998

Antigenic potential of DW-116, a newly synthesized fluoroquinolone, was examined by conduc-ting active systemic anaphylaxis (ASA), passive cutaneous anaphylaxis (PCA) and passive hemagglutination (PHA) tests. In ASA test, mild to moderate signs of anaphylactic responses were observed in the groups sensitized with low (2 mg/body) and high (10 mg/body) doses of DW-116 alone and the group sensitized with DW-116 plus adjuvant. Some moderate to severe anaphylactic reactions were observed in the group sensitized with a DW-116-bovine serum albumin (BSA) conjugate plus adjuvant when challenged with a DW-116-guinea pig senHn albumin (GSA) conjugate. However these reactions were considered to be a cross-reaction between BSA and GSA since similar reactions were induced when challenged by GSA alone. In heterologous PCA test using mice and rats, positive responses were not detected in any of the experimental groups. In PHA test, positive responses were observed in the groups sensitized with low and high doses of DW-116 alone and the group sensitized with DW-116 plus adjuvant. However, these responses were not considered to be drug-specific because some positive responses were also seen in the negative control group. From these results, it was concluded that DW-116 is not likely to have specific antigenic potential in clinical use.