• Title/Summary/Keyword: C3H

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Placental Transfer and Pharmacokinetics of a Single Oral Dose of the Fluoroquinolone Antibacterial DW-116 in Rats (랫드에서 fluoroquinolone 항균제 DW-116의 단회 경구투여에 의한 태반통과와 약물동태연구)

  • 김종춘;신호철;허정두;이종화;정문구;윤효인
    • Biomolecules & Therapeutics
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    • v.10 no.1
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    • pp.43-49
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    • 2002
  • The present study was conducted to investigate the placental transfer and pharmacokinetics of the flu-oroquinolone antibacterial DW-116 in pregnant rats. The placental transfer and pharmacokinetics of DW-116 were examined after a single oral dose of 500 mg $^{14}C$ DW-116/kg on gestational day 18. Maternal and fetal tissues were collected at 0.17 0.5,1,2,4,8, and 24 h after dosing. Maximum radioactivity was detected in maternal plasma, placenta, and whole fetus at 1 h, and in amniotic plasma at 4 h after dosing. Thereafter, radioactivity gradually disappeared from these tissues and was 16~28% of maximum levels at 24 h after dosing. Radioactivity in whole fetus were higher than those in the maternal plasma and placenta. The $T_{1/2,abs}$, $T_{1/2,{\beta}},$ AUC, $T_{max},$ and $C_{max}$ in the maternal plasma were approximately 6 min, 13.3 h, 1620 $ug^*hr/ml,$ 0.5 h, and 136 ug/ml, respectively. Those in the placenta were approximately 20 min, 12.3 h, 2150 $ug^*h/$m\ell$,$ 1.0 h, and 172 ug/ml, respectively. Those in the whole fetus were 13 min, 12.8 h,2549 $ug^*h/$m\ell$,$ 1 h, and 191 ug/ml, respectively. In the amniotic fluid of maternal uterus, the 4T_1/2,abs}$, $T1/2,{\beta},$ AUC, $T_{max},$ and $C_{max}$ were approximately 1.3 h,9.3 h,2508 $ug^*h/$m\ell$,$ 4.4 h, and 135 ug/ml, respectively. While DW-116 disappeared biphasically from maternal plasma, whole fetus and placenta, it was eliminated monophasically from amniotic fluid. In conclusion, this study demonstrated that the absorption and distribution of DW-116 in maternal plasma and placenta were extensively rapid, and that the test chemical well passed the blood-placenta barrier and was transferred to the fetus.

Preparation of Ni-doped Gamma Alumina from Gibbsite and Its Characteristics (깁사이트로부터 니켈피착 감마알루미나의 제조 및 특성)

  • Lee, Hyun;Chung, In-Sung;Park, Hee-Chan
    • Korean Journal of Materials Research
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    • v.8 no.12
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    • pp.1158-1164
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    • 1998
  • Aluminium sulfate solution was prepared by sulfuric acid treatment from gibbsite. Aluminium sulfate hydrate [$Al_2(SO_4)_3$ · $nH_2O$] was precipitated from aluminium sulfate solution by adding it into ethylalcohol. From XRD analysis as-prepared $Al_2(SO_4)_3$ · $nH_2O$ was confirmed to have mixed-crystalization water(n=18, 16, 12, 6). The average water of crystalization calculated from thermogravimetry(TG) was 14.7. Aluminium sulfate hydrate [$Al_2(SO_4)_3$ · $nH_2O$] was thermally decomposed and converted to $Al_2(SO_4)_3$ at $800^{\circ}C$, $\gamma-Al_2O_3$ at $900-1000^{\circ}C$, and $\alpha-Al_2O_3$ at $1200^{\circ}C$. Ni-doped $\gamma-Al_2O_3$, was synthesized from the slurry of as-prepared $\gamma-Al_2O_3$, with the ratio of [Ni]/[Al]=0.5. The reaction conditions of synthesis were determined as initial pH 9.0 and temperature $80^{\circ}C$ The basicity(pH) of slurry was controlled by using urea and $NH_4OH$ solution. Urea was also used for deposition-precipitation. For determining termination of reaction, the data acquisition was performed by oxidation reduction potential(ORP), conductivity and pH value in the process of reaction. Termination of the reaction was decided by observing the reaction steps and rapid decrease in conductivity. On the other hand, BET(Brunauer, Emmett and Teller) and thermal diffusity of Ni- doped $\gamma-Al_2O_3$, with various content of Ni were measured and compared. Thermal stability of Ni- doped $\gamma-Al_2O_3$ at $1250^{\circ}C$ was confirmed from BET and XRD analysis. The surface state of Ni-doped $\gamma-Al_2O_3$ was investigated by X-ray photoelectron spectroscopy(XPS). The binding energy at $Ni2P_{3/2}$ increased with increasing the formation of $NiAl_2O_4$ phase.

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Effect of Temperature on Removal of Ammonia in the Ceramic Biofilter Inoculated with Earthworm Casts (지렁이 분변토를 접종한 세라믹 바이오필터의 암모니아 제거에 미치는 온도의 영향)

  • Cho, Kyung-Suk
    • Journal of Environmental Impact Assessment
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    • v.9 no.1
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    • pp.39-46
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    • 2000
  • Removal of ammonia using the porous ceramic biofilter inoculated with earthworm casts was characterized. By assuming a plug air flow in the biofilter and applying the Michaelis-Menten equation, the maximum removal rate of $NH_3$ was $280.7g-N{\cdot}m^{-3}{\cdot}h^{-1}$($18.0g-N{\cdot}kg^{-1}{\cdot}d^{-1}$) at $30^{\circ}C$. $NH_3$ removal rate was increased as temperature increases from $15^{\circ}C$ to $35^{\circ}C$. The maximum removal rate was $285.8g-N{\cdot}m^{-3}{\cdot}h^{-1}$($18.8g-N{\cdot}kg^{-1}{\cdot}d^{-1}$) at $35^{\circ}C$. At $15^{\circ}C$, the $NH_3$ removal rate was $122.8g-N{\cdot}m^{-3}{\cdot}h^{-1}$($8.1g-N{\cdot}kg^{-1}{\cdot}d^{-1}$). When 210 ppm $NH_3$ was supplied to the biofilter at space velocity of $220h^{-1}$, the removal efficiency of $NH_3$ at 15, 25, 30 and $35^{\circ}C$ was 80, 90, 95, and 96%, respectively. The removal rate of the ceramic biofilter was 3 to 15 times higher than other biofilters comparing the removal efficiency of $NH_3$ per unit volume of carrier. This result indicates that earthworm casts and porous ceramics are very good inoculum source and carrier, respectively, for the $NH_3$-degrading biofilter.

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Theoretical Study of Acetic Acid-Sulfur Dioxide Complexes (Acetic Acid-Sulfur Dioxide 복합체에 대한 이론 연구)

  • Lee, Sang-Myeong;Sung, Eun-Mo
    • Journal of the Korean Chemical Society
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    • v.59 no.3
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    • pp.209-214
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    • 2015
  • The formation of complexes between SO2 and acetic acid was studied theoretically. The ab initio and DFT calculations were performed with MP2 and B3LYP methods using 6-311++G(d,p), aug-cc-pVDZ and aug-cc-pVTZ basis sets. Six stable complexes were identified, and three stable bidentate complexes, C1, C2 and C3, were formed between SO2 and syn-acetic acid, which is more stable form of acetic acid. Anti-acetic acid also form three complexes, C4, C5 and C6, with SO2. C4 is bidentate and C5, C6 are monodentate complexes, which are less stable. The most stable complex, C1 has S⋯O=C and O⋯H-O interactions, and the S⋯O and O⋯H distances are less than the sum of van der Waals radii. The vibrational frequencies of complexes were calculated and were compared with those of monomers. The frequency shifts after formation of complex were found, and the overall pattern of frequency shifts relative to monomers is similar among the six complexes.

Antifungal Activity of Polygodial against Food-Contaminants and Effects of Temperature and pH on the Action (Polygodial의 식품 오염 진균에 대한 항균 활성과 그 활성능에 미치는 온도 및 pH의 영향)

  • 이재란;이상화;홍순덕
    • Journal of Life Science
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    • v.8 no.4
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    • pp.421-425
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    • 1998
  • The antifungal activity of polygodial, which was isolated from Polygonum hydropiper used as a hot spice in Japan, was investigated through measuring its MICs and against food-contaminants including 4 strains of Saccharomyces cerevisiae, 3 strains of Zygosaccharomyces species, and 5 strains of Aspergillus species. All yeast-like fungi exhibited strong antifungal susceptivilities with MICs and MFCs below 3.13${\mu}g$/ml. Strains of Aspergillu species showed moderate with MIC of 25-50${\mu}g$/ml and MFC of 50-100${\mu}g$/ml. However these strains to sorbic acid, as already known, revealed very weak with MICs of 200-800${\mu}g$/ml and MFCs above 1600${\mu}g$/ml. In addition, effects of various pHs and temperatures on the antifungal activity of polygodial were tested against S. cerevisiae. At $4^{\circ}C$, the fungicidal activity of polygodial gradually increased with incubation time and reached the maximum(MFC of 3. 13${\mu}g$/ml) in 5 hours. At temperatures in the range of 30-$45^{\circ}C$, the activity of polygodial increased in proportion to temperature rise and in particular at $45^{\circ}C$ was possible with the concentration of 0.1${\mu}g$/ml. mOn the other hand, medium pH was also identified to affect the antifungal activity of polygodial. Namely, compared to neutral (pH7), acidic(pH 3) and basic(pH 9) medium synergized its activity (MIC and MFC) to 8- and 2- fold, respectively.

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Pullout capacity of shallow inclined anchor in anisotropic and nonhomogeneous undrained clay

  • Bhattacharya, Paramita
    • Geomechanics and Engineering
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    • v.13 no.5
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    • pp.825-844
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    • 2017
  • This study aimed to find out the pullout capacity of inclined strip anchor plate embedded in anisotropic and nonhomogeneous fully saturated cohesive soil in undrained condition. The ultimate pullout load has been found out by using numerical lower bound finite element analysis with linear programming. The undrained pullout capacity of anchor plate of width B is determined for different embedment ratios (H/B) varying from 3 to 7 and various inclination of anchor plates ranging from $0^{\circ}$ to $90^{\circ}$ with an interval of $15^{\circ}$. In case of anisotropic fully saturated clay the variation of cohesion with direction has been considered by varying the ratio of the cohesion along vertical direction ($c_v$) to the cohesion along horizontal direction ($c_h$). In case of nonhomogeneous clay the cohesion of the undrained clay has been considered to be increased with depth below ground surface keeping $c_v/c_h=1$. The results are presented in terms of pullout capacity factor ($F_{c0}=p_u/c_H$) where $p_u$ is the ultimate pullout stress along the anchor plate at failure and $c_H$ is the cohesion in horizontal direction at the level of the middle point of the anchor plate. It is observed that the pullout capacity factor increases with an increase in anisotropic cohesion ratio ($c_v/c_h$) whereas the pullout capacity factor decreases with an increase in undrained cohesion of the soil with depth.

The Production and Properties of Pretense by Serratia sp. 2000-1 Isolated from Clinical Specimes (임상검체에서 분리된 Serratia sp. 2000-1에 의한 Pretense의 생산 및 효소학적 성질)

  • 김태전;김승곤;김상택
    • Biomedical Science Letters
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    • v.6 no.3
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    • pp.209-221
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    • 2000
  • The purpose of this study was to investigate the practical availability of pretense production that can be used at home after isolating Serratia sp.2000-1 which produced extracellular pretense from clinical specimen. Basic production conditions and partial enzymatic characteristics of pretense produced by Serratia sp. 2000-1 was as follows: The kind and concentration of carbohydrate, nitrogen and metal salts for optimal enzyme production condition were each identified as the concentration of 1.5% glucose, 2.0% CSP, and 0.1% CaCl$_2$, and the optimal temperature, time and initial pH for culture were each 3$0^{\circ}C$, 72 hours, and pH 8.0. The final enzymatic yeild that was purified by 3 steps with ammonium sulfate precipitation (45~80%), DEAE-cellulose column chromatography, and Sephadex G-200 gel chromatography was 14.4%, and enzyme inactivity rate increased approximately 291314s. The optimal temperature and pH for purified pretense activity were 35$^{\circ}C$ and pH 7.0~8.0, and purified pretense activity was relatively stable by 4$0^{\circ}C$ at pH 6~10 for 30 min, however heating at 6$0^{\circ}C$ for 30 min, it liminated detectable pretense activity. The pretense activity was activated by $Mg^{2+}$, $Ba^{2+}$, $Ca^{2+}$, Mn$^{2+}$, but inactiviaed by Hg$^{2+}$, Ag$^{2+}$, Cu$^{2+}$, and the pretense activity was inhibited strongly by SDS among enzyme activity inhibitors. Further study is required to evaluate the practical availability of pretense production that can be used at home by isolating Serratia sp. from more clinical specimen and examining pretense more in details.

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Substituent Effect on Fragmentations and Ion-Molecule Reactions of Ionized Alkyn Alcohols

  • Choi, Sung-Seen;So, Hun-Young;Kim, Beom-Tae
    • Bulletin of the Korean Chemical Society
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    • v.26 no.4
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    • pp.609-613
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    • 2005
  • The fragmentation patterns and ion-molecule reactions of two alkyn alcohols, 2-propyn-1-ol (HC≡$CCH_2$OH) and 2-methyl-3-butyn-2-ol (HC≡CC($CH_3)_2$OH), were investigated using Fourier transform mass spectrometry (FTMS). The most abundant fragment ions formed from the molecular ions were [M-H]$^+$ for 2-propyn-1-ol and [M-$CH_3]^+$ for 2-methyl-3-butyn-2-ol. The dehydrated ion, [M-$H_2O]^+$ was formed only from 2-propyn-1-ol in which $\alpha$ -hydrogen atoms were available for $\alpha,\;\alpha$ -elimination reaction. The protonated molecules were dissociated into [M+H-$H_2O]^+$ and [M+H-$C_2H_2]^+$ through dehydration and deacetylenylation processes. The formations of [M+H-$H_2O]^+$ and [M+H-$C_2H_2]^+$ from 2-methyl-3-butyn-2-ol were more favorable than those from 2-propyn-1-ol due to stabilization by two methyl groups at $\alpha$ -carbon. Ion-neutral complexes formed at long ion trapping time gave dehydrated and/or deacetylenylated ion products by further dissociation.

One-pot Four Component Reaction of Unsymmetrical 1-Methylbarbituric Acid with BrCN and Various Aldehydes in the Presence of Et3N and/or Pyridine

  • Jalilzadeh, Mohammad;Pesyan, Nader Noroozi
    • Journal of the Korean Chemical Society
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    • v.55 no.6
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    • pp.940-951
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    • 2011
  • Reaction of 1-methylpyrimidine-(1H,3H,5H)-2,4,6-trione (1-MBA 1) as an unsymmetrical barbituric acid with cyanogen bromide and various aldehydes in the presence of triethylamine and/or pyridine afforded diastereomeric mixtures of new class of heterocyclic stable 5-aryl-1,1'-dimethyl- and 5-aryl-3,1'-dimethyl-1H,1'H-spiro[furo[2,3-d]pyrimidine-6,5'-pyrimidine]2,2',4,4',6'(3H,3'H,5H)-pentaones which are dimeric forms of 1-methyl barbiturate at the range of $0^{\circ}C$ to room temperature. In the reaction of some aldehydes with 1-MBA and BrCN were afforded a mixture of diastereomers. Another two aldehydes such as 4-cyano- and 2-hydroxybenzaldehydes gave exclusively two diastereomers in which binded to the salt of triethylammonium hydrobromide by intermolecular H-bond in ratio of 1:1. 4-Hydroxybenzaldehyde and 2-pyridinecarbaldehyde gave exclusively one diastereomer under the same condition. Aldehydes possessing strong electron-donor were produced exclusively two geometric isomers of Knoevenagel adduct (E- and Z-isomers). The structures of compounds were deduced by $^1H$ NMR, $^{13}C$ NMR and FT-IR spectroscopy. Mechanism of the formation is discussed.

Stability of pipethanate hydrochloride in aqueous solution

  • Kim, Chonng-Kook;Cha, Hyun-Sook
    • Archives of Pharmacal Research
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    • v.4 no.2
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    • pp.109-115
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    • 1981
  • In the present investigation, an attempt has been made to apply the methods of classical chemical kinetics to the hydrolytic reaction of pipethanate hydrochloride. By successively keeping all but one variable essentially constant, it has been possible to resolve the overall effect of the individual contributing factors. Since nearly all commercial pipethanate preparations are formulated with antacid, studies were made at several constant hydrogen ion concentration ranging pH 0.4 to 7.5. Rate measurement was also carried out in temperature ranging from $25^{\circ}C$ to $60^{\circ}C$. The hydrolysis of pipethanate is found to be of first order with respect to pipeethanate concentration over an experimental range of hydrogen ion concentration (pH 0407.5). The apparent activation energy(Ea) at pH 7.5 is 18.30 Kcal/mole and the frequency factor is $1.1408 {\times}10^{9}sec^{-1}$. The rate of the hydrolysis has a minimum at pH 2.5-3.5. In this region the half-life of pipethanate was about15.3 days at $60^{\circ}C$. The catalytic effect of water was found to be $K_{H_2O}$ = $3.16{\times}10^{-5}min^{-1}$ at $60^{\circ}C$. The catalytic constants of the hydroxyl ions and hydrogen ions at $60^{\circ}C$ were also found to be $K_{OH}$ = $4.5519{\times}10^{-5}min^{-1}$ and $K_{H}+$ = $1.1568{\times}10^{-2}min^{-1}$, respectively. This reaction appears to be primarily base catalyzed hydrolysis and pipethanate is relatively reluctant toward acid catalyzed hydrolysis. A positive primary salt effect was noted in the solution of phpethanate at pH 7.5 and at $60^{\circ}C$.

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