• YAKHAK HOEJI
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• v.36 no.6
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• pp.577-581
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• 1992

Norfloxacin complexes of $Fe^{2+}$, $Cu^{2+}$ and $Al^{3+}$ have been prepared as solids. The stoichiometry of the complexes has been established. IR investigation indicates the metal-ligating sites in norfloxacin. The bioactivities of complexes all lower than that of norfloxacin. The solubilities and partition coefficients have been measured as a function of temperature. The data are used to evaluate the thermodynamic parameters ${\Delta}G$, ${\Delta}H$, ${\Delta}S$ for the solute transfer process and compared with the parent quinolone, norfloxacin. The existence of such complexes is discussed in the light of quinolone mode-of-action theories.

• YAKHAK HOEJI
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• v.38 no.6
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• pp.721-724
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• 1994

According to computer graphics/Grid search analysis, ${\beta}-keto$ carboxylic acid of nalidixic acid which has an antibacterial activity as DNA-gyrase inhibitor has been known to have got four different conformational energy values. In orders, the energy value of conformation A,B,C and D was -6.603, -4.114, -1.766 and 7.327 kcal/mol. The difference of energy value between conformation A and D was 13.9 kcal/mol. Usually conformation C was used in literature. However, it had a energy value of -1.766 kcal/mol as the result of the analysis which is about 5 kcal/mol higher than the most stable conformation A. Therefore, conformation A is expected to be more stable than conformation C.

• YAKHAK HOEJI
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• v.43 no.4
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• pp.437-441
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• 1999

Enoxacin[1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-\piperazinyl)-1,8-naphthyridine-3-carboxylic acid, ENX] is a new quinolone antibacterial agent. The method is based on the highly colored charge-transfer complex formation of this drug as a $\pi$-electron donor with 7,7,8,8-tetracyanoquinodimethane(TCNQ) or chloranil(CL) as $\pi$-acceptors. The colored products were measured spectrophotometrically at 842 nm and 552 nm for TCNQ and CL, respectively. The different experimental conditions are optimized. The linearities for TCNQ and CL were $1.6{\;}\mu\textrm{g}/mL~32{\;}\mu\textrm{g}/mL$ and $6.4{\;}\mu\textrm{g}/mL~160{\;}\mu\textrm{g}/mL$, respectively and colors were produced in non-aqueous media. This report describes a simple and ra\pid method for the analysis of enoxacin.

• Bulletin of the Korean Chemical Society
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• v.17 no.2
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• pp.147-152
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• 1996

To see the quantitative relationship between the structures of the C-7 substituted quinolones and their antibacterial activities, theoretical parameters such as the molecular van der Waals volume, surface area and some electrostatic parameters based on the molecular electrostatic potential, which represent lipophilicity, and some quantum mechanical parameters are introduced as descriptors. The sixteen substituted quinolone derivatives and twenty bacteria are used for the study. It is found that the QSARs of C-7 substituted quinolones are obtained for eleven bacteria and our descriptors are more useful for Gram positive organisms than negative ones. It is also shown that molecular surface area (or molecular Waals volume) of the C-7 substituent and net charge of C-7 atom of the quinolones are the descriptors of utmost importance.

• Applied Chemistry for Engineering
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• v.34 no.2
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• pp.192-198
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• 2023

In this study, the components of microwave-assisted extracts obtained from Thuja orientalis leaves were analyzed, and the cytotoxicity, antibacterial and antiviral activities were evaluated. The predominant components from microwave-assisted extraction were catechin, leucopelargonidin, arecatannin, quinolone, and kaempferol derivatives, which are classified in the flavonoid and tannin groups. We observed that the 0.11 mg/mL of extract concentration did not show cytotoxicity in HaCaT cells. The antibacterial activities were tested according to the guidelines of methods for determining the bactericidal activity of antimicrobial agents. The extracts showed 99.9% antibacterial efficiency against gram-positive S. aureus, while the antibacterial effect on gram-negative E. coli was insignificant. When the extract concentration and contact time with bacteria were increased, 99.9% antibacterial efficiency was observed for E. coli as well as S. aureus. Following the standard to assess the activity of microbicides against viruses in suspension (ASTM-E1052-20), the antiviral efficiency was more than 99.99% for influenza A (H1N1) and SARS-CoV-2. These results suggest its potential use in antiviral disinfectants, surface coatings, personal protective equipment, and textiles.

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

• 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.

• Korean Journal of Veterinary Research
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• v.39 no.2
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• pp.365-369
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• 1999

A study on quinolone antibacterial, norfloxacin, was performed to apply for the control of bacterial diseases in eel (Anguilla japonica). Norfloxacin was proved excellent in antibacterial activity and sensitivity against fish bacterial pathogens when compared with the existing antibacterials and antibiotics. And any side effect was not observed during the period of indicated use. An outline of minimal inhibitory concentration was $0.03{\sim}0.1{\mu}g/ml$, $TLm_{48h}$ value was 3,500mg/l. The residual time of the day in fish body was less than 17 days and any pathological changes were not observed. The study has revealed that norfloxacin can be applied to treat some fish bacterial disease by the dosage of 100g/day/ton of fish body weight for about 3 days perorally. Further, norfloxacin may be used for the control of bacterial pathogens in eel.

• Proceedings of the Plant Resources Society of Korea Conference
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• 2018.10a
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• pp.113-113
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• 2018

Endophthalmitis is a disease that causes ocular inflammation and has a catastrophic effect on eyesight. Recent studies show that Enterococcus faecalis is rapidly increasing causative bacterium of endophthalmitis. It is predicted that the increased endophthalmitis by E. faecalis is presumable due to the high resistance of E. faecalis to moxifloxacin (MFX), which is a common antibiotic used for eye drop. Because of the need for therapeutic agents to overcome this problem, this study sought to explore the feasibility of developing a combination therapy using Orostachys japonicus. The ethylacetate fraction of O. japonicus (OJA) used in this study. Antimicrobial activity was tested 13 E. faecalis strains including one E. faecalis standard strain, eight clinically isolated E. faecalis strains and four quinolone resistant E. faecalis strains using CLSI antibiotic susceptibility test method. Minimal Inhibitory Concentration (MIC) of OJA was confirmed to be $500{\mu}g/ml$ for all 13 strains. Then we tested for the synergistic effect of OJA to MFX using checkboard test method. The MIC of MFX was $0.25{\mu}g/ml$ for the standard strain and 8 for the clinical isolates, and $16{\sim}64{\mu}g/ml$ for the quinolone - resistant strains. When OJA was mixed with MFX, no synergistic effect was observed in all strains, but the antibacterial activity of OJA remained unchanged. Most ocular other strains can be removed by MFX except the MFX resistant E. faecalis, which can be removed by OJA in combination therapy. Therefore, OJA can be a potential candidate for the combined treatment endophthalmitis.

• Biomolecules & Therapeutics
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• v.4 no.3
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• pp.239-243
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• 1996

DW-116 {(1-(5-fluoro-2-pyridyl)-6-fluoro-7-(4-methyl-1-piperazinyl)-1,4-dihydro-4-oxoquinoline-3-carboxylic acid hydrochloride) is a new quinolone antibiotic with a broad antibacterial spectrum against G(+) and G(-) bacteria. DW-116 was evaluated for the appearance of micronucleus in polychromatic erythrocytes (PCEs) of mouse bone marrow cells after intraperitoneal and oral single administration. We prepared the bone marrow cells at 30hr after drug administration and they were used for measuring PCE with micronucleus. The results showed there was no statistically significant increase in the numbers of PCEs with micronucleus in all DW-116 administered groups compared with a negative control group. The results also showed that the ratio of normochromatic erythrocytes(NCEs) to PCEs of all DW-116 administered groups was not significantly different from that of a negative control group. These results suggested that DW-116 may not cause any chromosomal damage and it has no in vivo mutagenic potential under these experimental conditions.