• Title/Summary/Keyword: S1P

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Synthesis of Cephalosporin Derivatives with Triazolylthiomethylpyrrolidines at the C-3 Side Chain (트리아조릴 티오메칠피로리딘을 3번 측쇄에 가진 세파로스포린 유도체의 합성)

  • 고옥현;홍준희
    • YAKHAK HOEJI
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    • v.46 no.5
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    • pp.313-319
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    • 2002
  • Synthesis of 7$\beta$-[(Z)-2-(2-aminothiazol-4-yl)-2-(1-carboxy-1-methylethoxyimino)acetamido]-3-[[(3S, 5S)-5-[4-phenyl-5-(4-methylphenyl or 2-thiophenyl)-4H-l, 2, 4- triazol-3-yl]thiomethylpyrrolidin-3-yl]]thiomethyl-3-cephem-4-carboxylic acids (7a, 7b) were described. (2S, 4S)-4-acethylthio-2-[4-phenyl-5-(4-methylphenyl or 2-thiophenyl)-4 H-1, 2, 4-triazol-3-yl]thiomethyl-1-tert-butoxycarbonylpyrrolidines (4a, 4b) were prepared from trans-4-hydroxy-L-proline with (2S, 4R)-absolute configuration as starting material. 4-Phenyl-5-(4-methylphenyl or 2-thiophenyl)-4 H-l, 2, 4-triazol-3-thiols (2a, 2b) were prepared from p-toluic anhydride and 2-thiophene carboxylic acid hydrazide, respectively. p-Methoxybenzyl 7$\beta$-(Z)-2-(2-for-mamidothiazol-4-yl)-2-(1-tert-butoxycarbonylisopropylimino]acetamido-3-[[ (3S, 5S)-5-[4-phenyl-5-(4-methylphenyl or 2-thio phenyl)-4H-1, 2, 3-triazol-3-yl]thiomethyl-1- tert-butoxycarbonylpyrrolidin-3-yl]]thiomethyl-3-cephem-4-carboxylates (6a, 6b) were achieved by using p-methoxybenzyl ]7P-(Z)-2-(2-formamidothiazol-4-yl)-2-(tert-butoxycarbonylisopropylimino] acetamido-3-chloromethyl-3-cephem-4-carboxylate (5) and (2S, 4S)-4-acethylthio-2-[4-phenyl-5-(4-methyl phenyl or 2-thiophenyl)-4H-1, 2, 4-triazol-3-yl]thiomethyl-1-tert-butoxycarbonyl pyrrolidines (4a, 4b). Removal of formyl, Boc, and p-methoxybenzyl protecting groups were carried out by triflu oroacetic acid and anisole to give the target compounds.

Study of Elastic Moduli of Sintered Low Alloy Steels by Acoustic Pulse Method

  • Hirose, Norimitsu;Oouchi, Kazuya;Fujiki, Akira;Asami, Junichi
    • Proceedings of the Korean Powder Metallurgy Institute Conference
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    • 2006.09a
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    • pp.387-388
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    • 2006
  • The influence of porosity (P) on Young's modulus (E) and Poisson's ratio $(\upsilon)$ of sintered steels produced from four types of steel powders was investigated. The values of E and $(\upsilon)$ depend mainly on the value of P, and those were a little affected by alloying elements. The relationships between E, $(\upsilon)$, and P were described as following equations: $E\;=\;E_0{\cdot}(1\;-\;k_E{\cdot}P)^2$ and $\upsilon\;=\;({\upsilon}_0\;-\;\upsilon_{sub}){\cdot}(1\;-\;k_{\upsilon}{\cdot}P)2+\upsilon_{sub}$, where subscript 0 means P = 0, and $k_E,\;k_{\upsilon}$ and ${\upsilon}_{sub}$ are empirical constants. These approximate equations showed good agreement with empirical results.

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Facile synthesis of optical pure fenoxaprop-p-ethyl[ethyl (R)-2-{4-(chloro-1,3-benzoxazol-2-yloxy)phenoxy}propionate] (광학활성 제초제 fenoxaprop-p-ethyl [ethyl (R)-2-{4-(6-chloro-1,3-benzoxazol-2-yloxy)phenoxy}propionate]의 새로운 합성법)

  • Ryu, Sung-Kon;Ko, Young-Kwan;Chang, Hae-Sung;Ryu, Jae-Wook;Woo, Jae-Chun;Koo, Dong-Wan;Kim, Dae-Whang;Chung, Kun-Hoe
    • The Korean Journal of Pesticide Science
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    • v.8 no.1
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    • pp.1-7
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    • 2004
  • Fenoxaprop-p-ethyl[Ethyl (R)-2-{4-(6-chloro-1,3-benzoxazol-2-yloxy)phenoxy}propionate] is well known as a herbicide for its specific activity against the weed grasses. This compound was synthesized by the reaction of 4-(6-chloro-1,3-benzoxazol-2-yloxy)phenol and ethyl (S)-O-(p-toluenesulfonyl)lactate in good yields with high optical pure(optical purity: 99.9% up). In this process Walden inversion occurs, whereby the S-configuration of the propionic acid derivative is converted to the R-configuration of the final product. 4-(6-Chloro-l,3-benzoxazol-2-yloxy)phenol was obtained by 5 step reactions in over-all 70% yields using inexpensive raw materials.

Inhibition of Apoptosis by Nitric Oxide in MCF-7 Cells (유방암 세포(MCF-7)에서 nitric oxide에 의한 apoptosis 억제)

  • Kim, Kyun-Ha;Roh, Sang-Geun;Park, Hae-Ryun;Choi, Won-Chul
    • Journal of Life Science
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    • v.19 no.2
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    • pp.157-162
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    • 2009
  • Nitric oxide (NO) is a diffusible, multifunctional and transcellular messenger that has been implicated in numerous physiological and pathological conditions. It has been reported that NO induced apoptosis in tumor cells, macrophage cells and inhibited apoptosis in normal cells, endothelial cells. To examine whether NO could induce apoptosis in MCF-7 cells, cells were treated with SIN-1 (3-morpholinosydnonimine), NO donor. Cell viability did not change in SIN-1 treated cells for 48 h and there was no significantly changes in cell cycle progression or growth pattern by FACS analysis. But p53 protein, an apoptosis-related factor, increased SIN-1 treatment time dependently. Bcl-2, MDM2 and p21 were also accumulated. Bax level did not change. A major role of inhibiting apoptosis by NO in MCF-7 cells, cobalt chloride ($CoCl_2$) was added to cells preincubated with SIN-1. Whereas $CoCl_2$ treated cells underwent apoptosis, for 24 h SIN-1 preincubated cells were not induced apoptosis. Inactivated proteins, MDM2 and bcl-2, by $CoCl_2$ levels also increased in SIN-1 pre-treated cells. These results suggested that SIN-1 blocked p53 by MDM2 activation and inhibited apoptosis by inducing p21 and bcl-2 expression.

Expression of Recombinant Human Cytochrome P450 1A2 in Escherichia coli Bacterial Mutagenicity Tester Strain

  • Chun, Young-Jin
    • Archives of Pharmacal Research
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    • v.21 no.3
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    • pp.305-309
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    • 1998
  • Human cytochrome P450 1A2 is one of the major cytochrome P450s in human liver. It is known to be capable of activating a number of carcinogens such as arylamines and heterocyclic amines. In order to develop the new bacterial mutagenicity test system with human P450, a full length of human P450 1A2 cDNA inserted into pCW bacterial expression vector was introduced to Escherichia coli WP2 uvrA strain which is a well-known E. coli strain for bacterial reverse mutagenicity assay. Expressed human P450 1A2 showed typical P450 hemoprotein spectra. Maximum expression was achieved at 48 hrs after incubating at $30^{\circ}C$ in terrific broth containing ampicillin, IPTG and other supplements. High level expression of P450 1A2 in E. coli WP2 uvrA membranes was determined in SDS-PAGE. The well-known mutagens 2-aminoanthracene and MElQ increased the revertant colonies of E. coli WP2 uvrA expressing human P450 1A2 without an exogenous rat hepatic post-mitochondrial supernatant (S9 fraction) in a dose-dependent manner. The results show that the functional expression of human P450 in bacterial mutagenicity tester strain will provide a useful tool for studying the mechanism of the mutagenesis and carcinogenesis of new drugs and environmental chemicals.

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Long-Term Feeding of Dietary Fat and Butylated Hydroxytoluene on The Hepatic Microsomal Mixed-Function Oxidase System in 2-Acetylaminofiuorene Treated Rats

  • Kim, Kyung-Min;Yim, Kyeong-Sook;Choi, Hay-Mie
    • Toxicological Research
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    • v.11 no.2
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    • pp.215-221
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    • 1995
  • This paper examines the effects of dietary polyunsaturated fatty acid/saturated fatty acid (p/s) ratios and butylated hydroxytoluene (BHT) on the hepatic microsomaI mixed-function oxidase sy. stem in 2~acetylaminofiuorene (2-AAF) treated rats. Sprague-Dawley male rats were fed the diet of beef tallow (p/s 0.08), beef tallow plus soybean oil (p/s 1.0), and soybean oil (p/s 4.0) at the level of 15%fat and with or without 0.3% BHT. After 2-AAF was injected twice at the ages of 23 and 27 weeks, cholesterol/phospholipid molar ratio, thiobarbituric acid reactive substances (TBARS) level, cytochrome P450, cytochrome $b_5$, NADPH-cytochrome $b_5$, and NADPH-cytochrome c reductase activity were measured from isolated hepatic microsomal fractions. In the beef tallow (p/s 0.08) and beef tallow plus soybean oil (p/s 1.0) groups, cholesterol/phospholipid molar ratio showed decreasing tendency by 2-AAF and BHT. Cytochrome P-450 content was decreased in the group of soybean oil (p/s 4.0) and NADPH-cytochrome c reductase activity was increased by 2-AAF and BHT in all the dietary groups. While TBARS levels were increased by 2-AAF in all the dietary groups, they were reduced by BHT in the soybean oil (p/s 4.0) group. These results suggest that long term intake of soybean oil (p/s 4.0) diet induced changes in the nature of microsomal membrane and induced less cytochrome P-450, low level feeding of BHT increased cytochrome c reductase activity and lowered microsomal lipid peroxidation levels, which were increased by 2-AAF treatment.

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Subcloning of Nodulin 26 Wild Type(S262) and Phosphorylation Site Mutant(S262D) into the Yeast Expression Vector pYES2

  • Cha, Youn-Soo
    • Preventive Nutrition and Food Science
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    • v.2 no.1
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    • pp.61-65
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    • 1997
  • Wild type nodulin 26(nod 26) cDNA(S262) and phodphorylation aite mutant(S262D) were constructed by a yeast expression system using pYES2 plasmids(pTES2-D262 and pTES2-S262D) were sc-reened by restriction mapping with BamHI of KpnI. S262 nod 26 contained a sreine residue at position 262 and S262D nod 26 contained the substitution mutation of serine to aspartic acid residue at position 262 were verified by automated floursent DNA sequencing.

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Comments on "Air Quality Impact Analysis of Point and Area Sources" ("점오염원과 면오염원의 대기환경영향 분석"에 대하여)

  • 김영성
    • Journal of Korean Society for Atmospheric Environment
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    • v.9 no.3
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    • pp.255-256
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    • 1993
  • Recently, Ghim and Son (1993) compared the air quality impacts of two point sources P1 and P3 in Seoul in the first quarter of 1988, whose emission rates were 99.9g/s and 49.4g/s, and whose stack heights were 75m and 21m. They said that higher concentrations from P3 in the nearby area were responsible for shorter stack height of P3. But concentrations were not raised so high only because the stack height was reduced from 75m to 21m. Volume of exit gas from P3 was also much smaller than that from P1.

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POLYNOMIALS THAT GENERATE A ROW OF PASCAL'S TRIANGLE

  • Kim, Seon-Hong
    • Communications of the Korean Mathematical Society
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    • v.17 no.3
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    • pp.383-387
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    • 2002
  • Let p be an odd prime, and let f($\varkappa$) be the interpolating polynomial associated with a table of data points (j+1, (equation omitted) ) for 0$\leq$j$\leq$p. In this article, we find congruence identities modulo p of (p-1)!f($\varkappa$), (p-2)!f($\varkappa$), and (p-3)!f($\varkappa$). Moreover we present some conjectures of these types.

Isolation of a Bacteriocin - Producing Lactobacillus sakei Strain from Kimchi (김치에서 박테리오신을 분비하는 Lactobacillus sakei균주의 분리)

  • 김한택;박재용;이강권;김정환
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.33 no.3
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    • pp.560-565
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    • 2004
  • Bacteriocin producing lactic acid bacteria (LAB) were isolated from Kimchi by using spot-on-the-lawn method. Listeria monocytogenes, Staphylococcus aureus, and Lactobacillus plantarum were used as indicators. One isolate (P3-l) produced a bacteriocin efficiently inhibiting the growth of Listeria monocytogenes. 16S rDNA sequence and sugar utilization test identified that P3-1 was a Lactobacillus sakei strain. Accordingly, the isolate was named as Lactobacillus sakei P3-1. L. sakei P3-1 produced a bacteriocin which efficiently inhibited the growth of Listeria monocytogenes but did not inhibit other Gram positive and negative organisms tested. The bacteriocin was stable against heat, organic solvent, and pH variation and it retained 50% of activity after 10 min heat treatment at 10$0^{\circ}C$. The molecular weight of Sakacin P3-1 was estimated to be 4 kDa by SDS-PAGE.