• YAKHAK HOEJI
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• v.37 no.3
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• pp.295-305
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• 1993

In order to develop oral cephalosporin having a new substituent at 3 position, the synthesis of cephalosporins modified at C-3 and the effect of the substituents on the oral absorption is studied. 7-[(Z)-2-(2-Aminothiazole- 4-yl)-2-methoxyiminoacetamidol-3-[4-(2-pyridyl )piperazinyl] thiocarbonylthiomethyl-3-cephem-4-carboxylic acid (CEN1) and 7-[(Z)-2-(2-aminothiazole-4-yl)-2-methoxyiminoacetamido]-3-[4-(2-pyrimid yl)piperazinylthiocarbonylthiomethyl-3-cephem-4-carboxylic acid (CEN2) were synthesized from 4-(2-piridyl)piperazinyl dithiocarbamate potassium salt or 4-(2-pirimidyl)piperazinyl dithiocarbamate potassium salt and cefotaxime. Also pivaloyloxymethyl esters of CEN1 and CEN2, pivaloyloxymethyl 7-[(Z)-2-(2-aminothiazole-4-yl)-2-methoxyiminoacetamido]-3-[4-(2-pyridyl )piperazinyllthiocarbonylthiomethyl-3-cephem-4-carboxylate (CENIP) and pivaloyloxymethyl 7-[(Z)-2-(2-aminothiazole-4-yl)-2-methoxyiminoacetamidol-3- [4-(2-pyrimid yl)piperazinyllthiocarbonylthiomethyl-3-cephem-4-carboxylate (CEN2P) were synthesized. The in vitro activities of two new oral cephalosporins, CEN1 and CEN2, were compared with the in vitro activities of cefaclor and cefotaxime against a variety of bacterial species. CEN2 has a broad antibacterial spectrum covering Gram-positive and Gram-negative bacteria, similar to that exhibited by CEN1 and cefotaxime. CEN1 and CEN2 were more active in vitro than cefaclor against Streptococcus pyogenes, Klebsiella aerogenes and Enterobacter cloacae.

• Journal of the Korean Chemical Society
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• v.38 no.7
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• pp.521-525
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• 1994

New cephalosporin antibiotics, 7-[(3,4-dihydro-6-methoxycarbonyl-2,2-dimethyl-2H-1,4-thiazin-3-yl)acetamido]-3-heterocyclothiomethyl-3-cephem-4-carboxylic acid derivatives(2a∼2d) were synthesized. Antibacterial activities of these new cephalosporin derivatives and the relationship between their structures and their activities were examined. Among them,7-[(3,4-dihydro-6-methoxycarbonyl-2,2-dimethyl-2H-1,4-thiazin-3-yl)acetamido]-3-[(2-methyl-1,3,4-thiadiazol-5-yl)thiomethyl]-3-cephem-4-carboxylic acid exhibited the broad antibacterial activities against Gram(+) and Gram(-) bacteria.

• YAKHAK HOEJI
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• v.42 no.4
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• pp.364-369
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• 1998

New cephalosporin antibiotics. 7-[(1H-tetrazolyl)acetamidol]-3-[(4-carboxy-3-hydroxyisothiazol-5-yl)thiomethyl-3-cephem-4-carboxylic acid trisodium salt 2,7-[(5-ethylthio-3-hydroxyisothiazol-4-yl)carbox-amidol-3-[(4-carboxy-3-hydroxyisothiazo1-5-yl)thiomethyl)-3-cephem-4-carboxylic acid 3,7-[(2-aminothiazol-4-yl)acetamido]-3-[(4-carboxy-3-hydroxyisothiazol-5-yl]thiomethyl]-3-cephem-4-caboxylic acid 4,7-[(Z)-2-(2-aminothiazol-4-yl)-2-(alkoxyimino)acetamido)-3-[(4-carboxy-3-hydroxyisothiazol-5-yl)thiomethyl)-3-cephem-4-carboxylic acid 5-9 were synthesized. Antibacterial activities of these new cephalosporin derivatives and the relationship between their structures and activities were examined. Among them, 7-((Z)-2-(2-aminothiazol-4-yl)-2-(carboxymethoxyimino)acetamido)-3-[(4-carboxy-3-hydroxyisothiazol-5-yl)thiomethyl)-3-cephem-4-carboxylic acid 8 and 7-[(Z)-2-(2-aminothiazol-4-yl)-2-(l-carboxy-1-methylethoxyimino)acetamido]-3-[(4-carboxy-3-hydroxyisothiazol-5-yl)thiomethyl)-3-cephem-4-carboxylic acid 9 exhibited good antibacterial activities compared with those of cefotaxime and ceftriaxone.

• YAKHAK HOEJI
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• v.41 no.4
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• pp.473-479
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• 1997

New cephalosporin antibiotics, 7-[(3,4-dihydro-6-methoxycarbonyl-2,2-dimethyl-2H-1,4-thiazin-3-yl)acetamido]-3-substituted-3-cephem-4-carboxylic acid derivatives 2a-2d, 7 -[(3,4-dihydro-6-ethoxycarbonyl-2,2-dimethyl-2H-1,4-thiazin-3-yl)acetamido] -3-substituted-3-cephem-4-carboxylic acid derivatives 3a-3d and 7-[(3,4-dihydro-6-methoxycarbonyl-2,2-dimethyl-2H-1,4-thiazin-3-yl-1-(S)-oxide)acetamido]-3-substituted-3-cephem-4-carboxylic acid derivatives 4a-4d were synthesized. Antibacterial activities of these new cephalosporin derivatives and the relationship between their structures and their activities were examined. Among them, 7-[(3,4-dihydro-6-methoxycaronyl-2,2-dimethyl-2H-1,4-thiazin-3-yl-1-(S)oxide)-acetamido]-3-[(1,2,3-triazol-5-yl)thiomethyl]-3-cephem-4-carboxylic acid 4d exhibited the antibacterial activities against Gram(+)and Gram(-) bacteria.

• YAKHAK HOEJI
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• v.44 no.4
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• pp.318-324
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• 2000

9 New cephalosporin derivatives were synthesized and screened for antibacterial activities against various bacteria. (6R,7R) -7$\beta$-[(Z)-2-(5-amino-1,2,4-thiadiazol-3-yl)-2-(fluoromethoxyimino)acetamido]-3-[(2-hydroxycarbamoyl)-s-triazolo[1,5-a]-pyrimidin-7-yl]thiomethyl]-3-cephem-4-carboxylic acid sodium salt (compound 3) showed 2 fold enhanced in vitro activity against P. aerurginosa, compared to ceftazidime.

• Natural Product Sciences
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• v.18 no.2
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• pp.137-140
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• 2012

The aim of this research was to investigate the industrial application of Zanthoxylum schinifolium. Antibacterial activities of the n-hexane, methylene chloride (MC), ethyl acetate, and butanol fractions of Z. schinifolium were tested against Escherichia coli, Staphylococcus aureus and Helicobacter pylori. Among the fractions, the n-hexane and MC fractions showed the stronger antibacterial activity against H. pylori, with an inhibition zone greater than 10 mm in disc assays. Further testing of bergapten and lupeol from the MC fraction of Z. schinifolium revealed the antibacterial effects against E. coli, S. aureus and H. pylori, suggesting their potential use as antibacterial agents.

• CELLMED
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• v.6 no.4
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• pp.22.1-22.19
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• 2016

The biologically active compounds derived from different natural organisms such as animals, plants, and microorganisms like algae, fungi, bacteria and merine organisms. These natural compounds possess diverse biological activities like anthelmintic, antibacterial, antifungal, antimalarial, antiprotozoal, antituberculosis, and antiviral activities. These biological active compounds were acted by variety of molecular targets and thus may potentially contribute to several pharmacological classes. The synthesis of natural products and their analogues provides effect of structural modifications on the parent compounds which may be useful in the discovery of potential new drug molecules with different biological activities. Natural organisms have developed complex chemical defense systems by repelling or killing predators, such as insects, microorganisms, animals etc. These defense systems have the ability to produce large numbers of diverse compounds which can be used as new drugs. Thus, research on natural products for novel therapeutic agents with broad spectrum activities and will continue to provide important new drug molecules.

• YAKHAK HOEJI
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• v.38 no.3
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• pp.265-273
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• 1994

ln vitro and in vivo antibacterial activities of DWQ-013(1-cyclopropyl-6,8-difluoro-7-(3-methylthiomethylpyrrolidinyl)-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid), a new fluoroquinolone antibacterial agent, were compared with those of ciprofloxacin, sparfloxacin and ofloxacin against aerobic and anaerobic standard strains and clinical isolates. DWQ-013 had a broad spectrum and potent antibacterial activity against Gram-positive and Gram-negative bacteria. The antibacterial activity of DWQ-013 against Staphylococcus aureus was equal to that of sparfloxacin(SPFX) and superior to those of ciprofloxacin(CPFX). The antibacterial activity against Gram-negative bacteria was slightly lower than those of ciprofloxacin and sparfloxacin. MIC of DWQ-013 against Pseudomonas aeruginosa$(0.781{\sim}1.563\;{\mu}g/ml)$ was usually equal to that of sparfloxacin$(0.781\;{\mu}g/ml)$ and was inferior to that of ciprofloxacin$(0.098\;{\mu}g/ml)$. The number of viable cells was decreased rapidly after addition of DWQ-013 at concentration of $1{\sim}2$ folds of MIC.

• The Journal of Advanced Prosthodontics
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• v.13 no.2
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• pp.100-106
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• 2021

PURPOSE. The purpose of this study is to compare the antibacterial activity of currently purchasable denture cleansers against Candida albicans. Materials and methods: This study used tablet-type denture cleansers, PolidentⓇ, CoolingdentⓇ and FittydentⓇ, along with liquid denture cleansers, HexamedineⓇ, ListerineⓇ and Apple vinegarⓇ. The antibacterial activities of denture cleansers were evaluated based on the number of C. albicans and concentrations of the denture cleansers. Results. In the 0.5 × 106 cfu/㎖ culture medium, the C. albicans' death rate of PolidentⓇ was significantly lower than those of FittydentⓇ, HexamedineⓇ, ListerineⓇ, and Apple vinegarⓇ(P<.05). In the 0.5 × 107 cfu/, the C. albicans' death rates of PolidentⓇ and CoolingdentⓇ were significantly lower than those of FittydentⓇ, HexamedineⓇ, ListerineⓇ and Apple vinegarⓇ(P<.05). The C. albicans' death rates of PolidentⓇ and CoolingdentⓇ were significantly decreased at 0.02 g and 0.01 g. The C. albicans' death rate of FittydentⓇ was significantly decreased at 0.005 g (P<.05). The C. albicans' death rate of HexamedineⓇ was significantly decreased at 1/16 dilution. The C. albicans' death rate of ListerineⓇ was decreased at 1/8 dilution, and the antibacterial activity of Apple vinegarⓇ was decreased at 1/4 dilution (P<.05). Conclusion. As the number of C. albicans increased, the antibacterial activities of the denture cleansers decrease. In the tablet-type denture cleanser, all denture cleansers showed 100% C. albicans' death rate when used at a dose of 1 tablet. One denture cleanser showed the same antibacterial effect with only 1/3 of a tablet. In the liquid type denture cleanser, the level of dilution required was different for each denture cleanser.

• Korean journal of food and cookery science
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• v.27 no.3
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• pp.21-28
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• 2011

In this study, we analyzed flower tea activity against oral bacteria. Lagerstroemia indica, Paeonia suffruticosa and Hemerocallis fulva showed high extract yields. Bellis perennis, Punica granatum and Cercis chinensis showed the high rates of yield by ethanol extraction. Extract yield seemed to be related to the characteristics of the specimens rather than to the solvent. Streptococcus mutans, Streptococcus obrinus, Porphyromonas gingivalis and Prevotella intermedia were used to investigate extracts activity against bacteria; the former two cause dental caries and the latter two cause halitosis. Cornus officinalis, L. indica, P. granatum and P.s uffruticosa showed high antibacterial activities against S. mutans. In specimens extracted with ethanol, P. suffruticosa, Camellia sinensis, Camellia japonica L. and Rosa hybrida showed high antibacterial activities. L. indica, P. granatum and C. officinalis showed high antibacterial activities against S. sobrinus. C. officinalis, P. granatum, L. indica and P. suffruticosa showed high activities for specimens extracted with ethanol. The results show that the warm extracts of C. officinalis, L. indica and P. granatum may be effective to prevent dental caries. In particular, the ethanol-based extracts of C. officinalis, P. suffruticosa and C. sinensis were effective to prevent dental caries and thus may be highly marketable. Chrysanthemum zawadskii, R. hybrida, P. granatum, C. japonica L. and Zinnia elegans showed high antibacterial activity against P.gingivalis. R. hybrida showed the highest ethanol extract activity, followed by P. suffruticosa, P. granatum, C. japonica L. and L. indica. R. hybrida, P. granatum, C. morifolium and C. japonica showed high activity against Pr.intermedia in the order named. C. zawadskii, P. granatum, L. indica, C. japonica and A. princeps showed high ethanol extract activity. Thus, the warm extracts of R. hybrida, P. granatum and C. japonica may be helpful to reduce halitosis. In addition, the ethanol-based extracts of P. granatum, C. japonica and L. indica are expected to be highly marketable as mouthwashes.