• Journal of Microbiology and Biotechnology
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• v.26 no.1
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• pp.56-60
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• 2016

Two new glucosides (1 and 2) of geldanamycin (GA) analogs were obtained from in vitro glycosylation by UDP-glycosyltransferase (YjiC). Based on spectroscopic (HR-ESI-MS, 1D, and 2D-NMR) analyses, the glucosides were elucidated as 4,5-dihydro-7-O-descarbamoyl-7-hydroxyl GA-7-O-β-D-glucoside (1) and ACDL3172-18-O-β-D-glucoside (2). Furthermore, the water solubility of compounds 1 and 2 was about 215.2 and 90.7 times higher respectively, than that of the substrates. Among compounds 1-4, only 3 showed weak antiproliferative activity against four human tumor cell lines: MDA-MB-231, SMMC7721, HepG2, and SW480 (IC₅₀: 13.6, 15.1, 31.8, and 22.7 μM, respectively).

• Biomolecules & Therapeutics
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• v.5 no.4
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• pp.419-425
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• 1997

The pharmacokinetics of DWP20364 (1-cyclopropyl -5-amino-6,8-difluoro-7-(2,7-diazabiclo [3,3,0] oct-4-ene-7-yl)-1,4-dihydro-4-oxoquinoline-3-carboxylic acid), a novel fluoroquinolone containing C7-bicyc-talc structure, were compared with those of ciprofloxacin (CPFX) after single intravenous (i.v.) and oral (p.o.) administration to rats using microbiological assay (bioassay). After i.v. administration to rats, the plasma concentrations of the two drugs declined biexponentially. The terminal half-lives (t$_{1}$2$\beta$/) of DWP20364 were 110$\pm$ 13.2 min and 117$\pm$3.09 min after i.v. and p.o. administration, respectively, and they were significantly higher than those of CPFX (45.5$\pm$9.52 min and 48.3$\pm$ 12.1 min, respectively). Similar results were also obtained from plasma concentrations and area under the plasma concentration-time curves. The total body clearance of DWP20364, 7.82$\pm$0.37 ml/min/kg was significantly slower than that of CPFX, 27.3 $\pm$ 11.1 m1/ min/kg. Above data suggested that the antimicrobial activity of DWP20364 could be longer than that of CPFX. The urinary recovery after i.v. and p.o. administration of DWP20364 was significantly lower than those of CPFX suggesting that the effect of DWP20364 on urinary tract infection could be lower than that of CPFX. The serum protein binding values of DWP20364 at 2$\mu$g/ml were apparently 91.5~93.1% in rats and human. DWP20364 was distributed by the order of liver, lung, kidney, sf)leon, heart, muscle and brain collected at 30 min after orally administered.

• Journal of the Korean Society of Food Science and Nutrition
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• v.35 no.7
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• pp.881-885
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• 2006

The product formation and changes in color of glucose/glutamine model system were investigated in relation to heating temperature and time. The mixtures of glucose and glutamine in equal molar ratio were heated at 125, 150 and $175^{\circ}C$ for 10, 20 and 30 minute, respectively. Acetic acid, butanoic acid, 2-butenoic acid, di-(2-cthylhexyl)phthalate, 2,3-dihydro-3,5-dihydroxy-6-methly-4H-pyran-4-one and 5-hydroxymethylfurfural were identified as a major compounds, and 1,3-dimethylbenzene, 2-ethylhexanol, furfural, 5-methylfurfural, 2-pyrrolidinone, and 2,6-di(t-butyl)-4-hydroxy-4-methyl-2.5-cyclohexadien-1-one as 6 minor compounds by using GC/MS. The contents of acetic acid, 2-ehylhexanol and 2-pyrrolidinone increased with increased heating temperature and time, whereas the formation of the other 9 compounds increased up th heating conditions of $150^{\circ}C$ for 10 or 20 min or $175^{\circ}C$ for 10 min, and decreased dramatically with heating above those conditions. Color parameter $L^*$ decreased with increasing heating conition, resulting in dark brown color in final products. Changes of redness parameter $a^*$ and yellowness $b^*$ showed similar to those of the contents of 9 compounds mentioned as above.

• Journal of the Korean Institute of Electrical and Electronic Material Engineers
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• v.23 no.7
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• pp.539-544
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• 2010

We have synthesized new blue electroluminescent polyalkylfluorene-based copolymers [poly(F-co-Py)x:y, where x:y = 99:1 or 95:5 mole ratios] containing the hole-injecting pyrazole derivative [3,3'-(4,6-bis(octyloxy)-1,3-phenylene)bis(1,5-diphenyl-4,5-dihydro-1H-pyrazole] through Ni(0) mediated polymerization, and their electroluminescent properties were investigated. Electroluminescent (EL) devices were fabricated with ITO / PEDOT:PSS (110 nm) / copolymers or PF homopolymer (80 nm) / Ca (50 nm) / Al (200 nm) configuration. Each EL device constructed from the copolymer exhibited significantly enhanced brightness and efficiency compared with a device constructed from the PF homopolymer. The EL device constructed with poly(F-co-Py)99:1 exhibited the highest luminous efficiency and brightness (0.95 cd/A and $2,907\;cd/m^2$, respectively). The achieved luminous efficiency was an excellent result, providing almost a 4-fold improvement on the efficiency obtainable with the a PF homopolymer device. This enhanced efficiency of the copolymer devices results from their improved hole injection and more efficient charge carrier balance, which arises from the HOMO level (~5.83 eV) of the poly(F-co-Py)99:1 copolymer, which is higher than that of the PF homopolyme (~5.90 eV).

• Biomolecules & Therapeutics
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• v.11 no.4
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• pp.232-237
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• 2003

The present study examined functional effects of a new selective phosphodiesterase type 5 inhibitor, 1-[4-ethoxy-3-(6,7-dihydro-1-methyl-7-thioxo-3-propyl-1H-pyrazolo[ 4,3]pyrimidin-5-yl)phenylsulphonyl]-4-methyl piperazine (KJH-1002), in the isolated rabbit corpus cavernosum (RCC). Relaxing effects of KJH-1002 were also compared with those of sildenafil, which is currently used as an oral therapy for penile erectile dysfunction. In the isolated RCC precontracted with phenylephrine, both KJH-1002 and sildenafil in the concentration range of 1 to 1000 nM, produced a comparable potentiation of the electical field stimulation-induced relaxation in a concentration-dependent manner. In the sodium nitroprusside (SNP)-induced relaxation, the $IC_{50}$/ values, concentrations of SNP required to produce a 50％ relaxation of the phenylephrine-induced contraction, were significantly decreased to the similar extent by treatments with KJH-1002 and sildenafil. The results suggest that a new selective phosphodiesterase type 5 inhibitor, KJH-1002, has an augmentative effect on penile erection comparable to that of sildenafil and can be useful for the treatment of erectile dysfunction.

• Journal of the Korean Wood Science and Technology
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• v.30 no.4
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• pp.74-79
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• 2002

Three different kinds of the crude vinegars obtained from oak(Quercus serrata), bamboo(Phyllostachys pubescens) and pine(Pinus densiflora) species were stored for approximately one year and periodically analyzed to monitor their physicochemical changes. Small changes in physical properties, such as the pH, specific gravity and amount of organic acids as well as water-soluble tar were observed in the entire course of aging period. However, the color difference of the vinegars showed a remarkable change between 7 and 10 months. In addition, these vinegars' colors changed from light yellowish orange to much deeper purple and orange during this period. The amount of organic acids and neutral compounds(dihydro-2(3H)-furanone, furfural, furfuryl alcohol, 2-hydroxy-1-methyl-1-cyclopenten-3-one, 1-hydroxy-2-propanone and methanol) in the vinegars increased or decreased periodically every three months. A good linear relationship (correlation coefficient of ca. 0.92) was obtained between the amount of organic acids and the amount of neutral compounds in such changes. However, although the amount of phenols increased or decreased periodically, its amount was decreased over the entire aging.

• Bulletin of the Korean Chemical Society
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• v.31 no.7
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• pp.1976-1980
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• 2010

A simple and reliable method has been developed to selectively separate and concentrate trace amounts of Fe(III) ions from water and food samples by using flame atomic absorption spectrometry. A new reagent, 5-hydroxy-4-ethyl-5,6-di-pyridin-2-yl-4,5-dihydro-2H-[1,2,4] triazine-3-thione, was synthesized and characterized by using FT-IR spectroscopy and elemental analysis. Effects of pH, concentration and volume of elution solution, sample flow rate, sample volume and interfering ions on the recovery of Fe(III) were investigated. The optimum pH was found to be 5. Eluent for quantitative elution was 10 mL of 2 M HCl. The preconcentration factor of the method, detection limit (3s/b, ${\mu}gL^{-1}$) and relative standard deviation values were found to be 25, 4.59 and 1%, respectively. In order to verify the accuracy of the method, two certified reference materials (TMDA 54.4 lake water and SRM 1568a rice flour) were analyzed. The results obtained were in good agreement with the certified values. The method was successfully applied to the determination of Fe(III) ions in water and food samples.

• Journal of the Korean Society of Clothing and Textiles
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• v.34 no.6
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• pp.1042-1052
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• 2010

The Degradation of amur cork tree extract is investigated by GC-MS after treating the dye with three thermal degradation systems of, room temperature (RT), $4^{\circ}C$ refrigeration (LT), $100^{\circ}C$ oven (OV), and $H_2O_2$/UV/$O_2$ (PER) degradation system for 0-24 days. It was found that PER degradation system represented the highest intensity of degradation treatment followed by OV treatment among the four degradation parameters. The possible fingerprint products of amur cork tree dye, that yielded 68% (or higher) reliability in the NIST spectral match, were isobenzofuran-1,3-dione,4,5-dimethoxy- (8.37 min, PER only), 1,3-dioxolo[4,5-g]isoquinolin-5(6H)-one,7,8-dihydro (9.41 min, PER only), canthine-6-one (10.24 min, RT, LT, OV only), and dihydroberberine (15.05 min, RT, LT, OV, PER) in the order of higher to lower possibility of detection. Unknown products 7 (13.43 min) and 8 (16.35 min) are two other possible fingerprint products of amur cork tree dye that require future identification.

• 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.

• Bulletin of the Korean Chemical Society
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• v.35 no.2
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• pp.617-621
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• 2014

An efficient and selective method for the synthesis of ethyl 2-amino/aryloxy-3-aryl-4-oxo-5-phenyl-4,5-dihydro-3H-pyrrolo[3,2-d]pyrimidine-7-carboxylate derivatives has been developed. The main process involved the reaction of diethyl 1-phenyl-3-((triphenylphosphoranylidene)amino)-1H-pyrrole-2,4-dicarboxylate and aromatic isocyanates, followed by addition of amines/phenols in the presence of catalytic amount of sodium ethoxide or solid potassium carbonate.