• YAKHAK HOEJI
• /
• v.52 no.3
• /
• pp.219-224
• /
• 2008

Clinically isolated methicillin-resistant Staphylococcus aureus strains were exposed to subinhibitory concentration of DW286, DW-224a, gemifloxacin, trovafloxacin, sparfloxacin and ciprofloxacin during 26- to 39-days period. Subculturing led to resistance development, and most of the selected mutants were above susceptible breakpoints. Selected mutants had broad cross resistance to other quinolone antibiotics and only one mutant was completely susceptible to all fluoroquinolones. Twenty five among 42 mutants revealed mutations on DNA gyrase and topoisomerase IV by sequencing. Also 16 mutants had fluoroquinolones MICs that were 4-32 times lower in the presence of reserpine. In conclusion, alterations in DNA gyrase or topoisomerase IV and action of efflux pumping out system are the resistance mechanisms of DW-224a.

• YAKHAK HOEJI
• /
• v.38 no.5
• /
• pp.586-594
• /
• 1994

The general pharmacological effects of DWQ-013, a new synthetic quinolone antibacterial agent, were examined on the central nervous system in experimentral animals and the following results were obtained. Drug interaction of DWQ-013 with theophylline, fenbufen and nonsteroidal antiinflammatory drugs was also examined. DWQ-013 decreased touch escape effect on the general behavior and decreased body temperature at a concentration of 1000 mg/kg in mice. But DWQ 013 had no effect on the locomotor activity, rotarod perfomance and traction test in mice. Furthermore, DWQ-013 increased pentobarbital-induced sleeping time and affected the onset time in acetic acid-induced writhing test in mice. DWQ-013 reduced onset time and death time on strychnine-induced convulsions and death time on pentylenetetrazole-induced convulsions at a concentration of 1000 mg/kg in mice. But, the drug had no effect on the electroshock. DWQ-013 did not interact with fenbufen and any other NSAIDs but it did interact with theophylline. From these results, it could be suggested that DWQ-013 had less pharmacological effect than other quinolones on the central nervous system.

• Korean Journal of Veterinary Service
• /
• v.36 no.4
• /
• pp.311-320
• /
• 2013

The purpose of this study was to evaluate detecting methods and the relationship between tissues and blood for enrofloxacin and metabolic ciprofloxacin residues in broiler chickens. Two groups of broiler chickens were administrated via the drinking water with $50{\mu}g/mL$ and $100{\mu}g/mL$ of enrofloxacin for 5 days, respectively. The concentration of enrofloxacin and metabolic ciprofloxacin in tissues (muscle and kidney) and blood were measured during administration period (for 5 days) and withdrawal period (for 12 days) by high performance liquid chromatography (HPLC) method. Also, all samples were conducted for screening of residues by microbial method using E. coli for quinolone detection and immuno-chromatography method using Smart kit. The relationship between tissues (muscle and kidney) and blood for enrofloxacin and metabolic ciprofloxacin residues in broiler chickens was followed : The levels of enrofloxacin and metabolic ciprofloxacin residues in muscle and kidney were higher 2.9~3.2 folds, 3.6~3.8 folds more than the residues levels in blood, respectively. These results support we can predict the residues in muscle and kidney from the residues in blood. In comparison of detecting methods for antibiotic residues, microbial method using E. coli for quinolone detection and immuno-chromatography method using Smart kit could detect positive reaction at similar or lower concentration than violative concentration of enrofloxacin and metabolic ciprofloxacin in chicken tissues. These results support what two screening methods are useful for screening of quinolone detection in chickens.

• YAKHAK HOEJI
• /
• v.45 no.4
• /
• pp.334-338
• /
• 2001

A series of (-)-9-fluoro-2,3-dihydro-3(S)-methyl-10-(4-substituted-1-piperazinyl)-7-oxo-7H-pyrido [1,2,3-de] [1,4]-benzoxazine-6-carboxylic acid (5-8) was synthesized and evaluated for antibacterial activity against gram(+) and gram(-) bacteria. These synthesized compounds showed a lower activity than levofloxacin.

• Bulletin of the Korean Chemical Society
• /
• v.29 no.11
• /
• pp.2103-2108
• /
• 2008

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

• Bulletin of the Korean Chemical Society
• /
• v.11 no.5
• /
• pp.376-379
• /
• 1990

To find out a correlation between antibacterial activity and physical properties of 7-substituted 1-ethyl-6-fluoro-1,4-dihydro-4-oxoquinoline-3-carboxylic acid, dipole moments, charge distributions, and hydrophobicities were calculated. The atomic charges and the dipole moments to not give any correlations with inhibition of DNA gyrase, but the calculated hydration free energies show some correlations.

• Bulletin of the Korean Chemical Society
• /
• v.19 no.6
• /
• pp.667-671
• /
• 1998

A series of 1-aryl-lH-pyrazolo[4,3-c]quinolines and 2-aryl-2H-pyrazolo[4,3-c]quinolines are prepared by reacting 3-acyl-4-chloroquinolines in ethanol or 3-acyl-4(lH)-quinolone in acetic acid with appropriate hydrazines as possible anti-ulcer agents. A regiospecific synthesis of 1-aryl-lH-pyrazolo[4,3-c]quinolines is also achieved. The central pyridine ring could be easily reduced by catalytic hydrogenation.

• Bulletin of the Korean Chemical Society
• /
• v.11 no.4
• /
• pp.313-317
• /
• 1990

Geometries for several representative quinolone carboxylate type antibacterials have been calculated by computer graphics/molecular mechanics energy minimization procedures using both MM2 and AMBER force fields. The calculated geometries were found to be in reasonable agreements with the corresponding X-ray crystal structures. It has been pointed out that notwithstanding the weaknesses associated with calculating the resonance and hydrogen bonding contributions, the employed methods are capable of generating credible ring geometries and torsional angle dispositions of N(1)-ethyl and 3-carboxylate substituents of the quinolones.

• Biomolecules & Therapeutics
• /
• v.6 no.1
• /
• pp.73-81
• /
• 1998

Pregnant Sprague-Dawley rats were administered with Q-35 at the dose levels of 0, 30, 100 and 300 mg/kg/day by oral gavage from gestation day 17 to lactation period. Effects of the test chemical on general findings, reproductive performance of dams and development of Fl generation were examined. There were no treatment related changes in physical signs, body weight, necropsy findings, organ weights, delivery and nursing behavior. In 100 and 300 mg/fg/day treated groups, the food consumption of dams was decreased significantly during gestational day 19~21. The gestation length of 300 mg/tg/day treated group was increased significantly compared to the control group (22.3 $\pm$0.48 vs 22.0$\pm$0.39). Although the gestational length of all groups were in normal range of the rat, potential effect of the drug could not be ruled out. External anomaly of Fl fetus induced by Q-35 was not detected in any groups. There were no treaoent related changes in physical development, reflex functions, sensory functions, locomotor activity and motor coordinating activity. Estrus cycle, fertility and reproductive performance of Fl were not changed in all treated groups. There was no external abnormality related to the drug administration on the examination of F2. These results suggest that Q-35 has no adverse effect on the peri- and postnatal period in rats except the reduction of food consumption at the beginning of drug administration and the potential effect on the elongation of gestation length.