• Title/Summary/Keyword: Substituted

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Synthesis and Biological Effects of 2, 3-Diphenyl-5-Methoxyindole and Substituted Benzophenone Derivatives

  • Hishmat, O.H.;El-Sbabrawy, O.A.;Nakkady, S.S.;Mahmoud, S.S.
    • Archives of Pharmacal Research
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    • v.12 no.3
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    • pp.149-153
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    • 1989
  • Seven 2, 3-diphenyl-5-methoxyindole derivatives were synthesized. The effect of structural variation of these molecules on biological activities was examined. None of the tested compounds was found to be toxic up 5 gm/Kg body weight. Four compounds demonstrated smooth muscle relaxant effects and one showed a persistent hypotensive effect. Only the parent compound, 2, 3-diphenyl-5-methoxyindole, showed a significant analgesic effect.

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Novel Inhibitors of Prolyl 4-Hydroxylase; Solid-phase Synthesis of 2,2-Dimethyl-3,4-Dialkoxy-Substituted 6-Aminobenzopyran Derivatives

  • Seo, Jin-soo;Joo, Yang-Hee;Yi, Jung-Bum;Lee, Eun-Ju;Lee, Nam-Kyu;Cho, Yong-Balk;Kwak, Wie-Jong;Hwang, Jong-Yeon;Jeon, Yong-Seog;Jeon, Hyun-Suk;Yoo, Sung-eun;Yoon, Cheol-Min;Dong, Mi-Sook;Gong, Young-Dae
    • Bulletin of the Korean Chemical Society
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    • v.27 no.6
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    • pp.909-917
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    • 2006
  • 2,2-Dimethyl-3,4-dialkoxy-substituted 6-aminobenzopyran analogues (eg., 7 and 8) were identified as prolyl 4-hydroxylase inhibitors via a screening process using HSC-T6 and LI 90 cells that express an immortalized rat hepatic stellate cell line and as part of a test of the type I collagen contents employing the ELISA method. A subsequent lead optimization effort based on solid-phase parallel synthesis led to the identification of 2,2-dimethyl-3,4-dialkoxy-substituted 6-aminobenzopyrans as potent inhibitors of prolyl 4-hydroxylase.

Synthesis and Characterization of Substituted Pyridine Complexes of Molybdenum (Ⅳ). Oxotrichlorobis(substituted pyridine) molybdenum (Ⅴ) (몰리브덴의 피리딘계 착물합성과 그 성질 (제4보) 옥소삼클로로비스(치환피리딘)몰리브덴 (V))

  • Chang Su Kim;Sang Oh Oh
    • Journal of the Korean Chemical Society
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    • v.26 no.6
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    • pp.378-382
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    • 1982
  • Green crystalline salts of substituted pyridinium oxopentachloromolybdates(V) were obtained from concentrated hydrochloric acid solution of molybdenum(V)-thiocyanate extract. $MoOCl_3(X-py)_2$ (X-py were 4-and 3-cyanopyridine, 2-amino-4-picoline and 4-acetylpyridine) were obtained by reflux of the corresponding substituted pyridinium salts of oxopentachloromolybdates(Ⅴ) in absolute ethanol. ($X-pyH_2$)[$MoOCl_5$]$H_2$O containing the $MoO^{3+}$ group are dissolved and hydrolysed in water but $MoOCl_3(X-py)_2$ are insoluble in water, alcohol and acetone. The complexes are paramagnetic compounds.

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Synthesis of Hydrazone Derivatives of 4-(2-Chloroethyl) semicarbazide : A New Class of Cytotoxic Agents (4-(2-Chloroethyl) semicarbazide의 히드라존 유도체 합성:새로운 종류의 세포독성요법제)

  • El-Sabbagh, O.I.;El-Sadek, M.E.;Aboukull, M.E.;Shallal, H.M.
    • Journal of the Korean Chemical Society
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    • v.53 no.1
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    • pp.34-41
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    • 2009
  • A new series of hydrazone derivatives were synthesized from 4-(2-chloroethyl)semicarbazide and their antiproliferative activity against human brain (U251) and liver (Hepg2) carcinoma cell lines were evaluated. The hydrazone compounds are benzaldehyde (2a-2g), acetophenone (3a-3f), and 3-formylindole derivatives (4a-4d). Among the acetophenone derivatives, 3e (p-methoxy substituted) and 3f (p-nitro substituted) showed the highest cytotoxic activity against Hepg2 cell line (I$C_{50}$ = 6 and 8 $\mu$g/ml, respectively). Among the 3-formylindole derivatives, 4a (hydrazone of 3-formylindole itself) showed a pronounced cytotoxic activity against both U251 (I$C_{50}$ = 21 $\mu$g/ml) and Hepg2 (I$C_{50}$ = 7 $\mu$g/ml).

New Gene Cluster from Thermophile Bacillus fordii MH602 for Conversion of DL-5-Substituted Hydantoins to L-Amino Acids

  • Mei, Yan-Zhen;Wan, Yong-Min;He, Bing-Fang;Ying, Han-Jie;Ouyang, Ping-Kai
    • Journal of Microbiology and Biotechnology
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    • v.19 no.12
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    • pp.1497-1505
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    • 2009
  • The thermophile Bacillus fordii MH602 was screened for stereospecifically hydrolyzing DL-5-substituted hydantoins to L-$\alpha$-amino acids. Since the reaction occurs at higher temperature, the advantages for enhancement of substrate solubility and for racemization of DL-5-substituted hydantoins during the conversion were achieved. The hydantoin metabolism gene cluster from thermophile is firstly reported in this paper. The genes involved in hydantoin utilization (hyu) were isolated on an 8.2-kb DNA fragment by restriction site-dependent PCR, and six ORFs were identified by DNA sequence analysis. The hyu gene cluster contained four genes with novel cluster organization characteristics: the hydantoinase gene hyuH, putative transport protein gene hyuP, hyperprotein gene hyuHP, and L-carbamoylase gene hyuC. The hyuH and hyuC genes were heterogeneously expressed in E. coli. The results indicated that hyuH and hyuC are involved in the conversion of DL-5-substituted hydantoins to an N-carbamyl intermediate that is subsequently converted to L-$\alpha$-amino acids. Hydantoinase and carbamoylase from B. fordii MH602 compared respectively with reported hydantoinase and carbamoylase showed the highest identities of 71% and 39%. The novel cluster organization characteristics and the difference of the key enzymes between thermopile B. fordii MH602 and other mesophiles were presumed to be related to the evolutionary origins of concerned metabolism.

Effects of 1,7-Substituted Methylxanthine Derivatives on LPS-Stimulated Expression of Cytokines and Chemokines in Raw 264.7 and HK-2 Cells

  • Kang, Joo-Yeon;Shin, Hea-Soon
    • Journal of Microbiology and Biotechnology
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    • v.25 no.2
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    • pp.296-301
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    • 2015
  • Chronic kidney diseases are based on uncontrolled immunological and inflammatory responses to pathophysiological renal circumstances such as glomerulonephritis, which is caused by immunological mechanisms of glomerular inflammation with increased production of renal pro-inflammatory cytokines. Pentoxifylline (PTX) exhibits anti-inflammatory properties by inhibiting cytokine and chemokine production through aggregation of erythrocytes and thrombocytes. We synthesized a series of 1,7-substituted methylxanthine derivatives by the Traube purine reaction, and the formation of purine ring was completed through nitrosation, a reduction of the nitroso to the amine by catalytic hydrogenation as derivatives of PTX. Then we studied biological activities such as renal anti-inflammatory effects of the synthesized compounds in the production of cytokines such as nitric oxide (NO), interleukin (IL)-1β, IL-6, and tumor necrosis factor-α (TNF-α) and of chemokines such as monocyte chemoattractant protein-1 and IL-8 in Raw 264.7 and HK-2 cells. Renal antiinflammatory activities of this novel series of N-1 and N-7-substituted methylxanthine showed that the N-7 methyl-group-substituted analogs (S7b) showed selective 61% and 77% inhibition of the production of NO and IL-8. The other replacement of the N-1-(CH2)4COCH3 roup, as in the case of compound S6c, also showed an effective 50% and 77% inhibition of TNF-α and IL-8 production in LPS-stimulated Raw 264.7 and HK-2 cells.

Synthesis and Crystal Structure of Asymmetric Dimer of 1,2-Benzothiazine Derivatives Using Silver Oxide (Silver Oxide를 이용한 1,2-벤조티아진 유도체의 비대칭 중합체 합성 및 결정 구조)

  • Park, Myung Suk
    • Journal of the Korean Chemical Society
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    • v.42 no.6
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    • pp.657-663
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    • 1998
  • New asymmetric dimer, 7,7'-substituted (or H)-4-oxo-2,2'- dialkyl-l,l',2,2'-dibenzothiazine-3,3'dicarboxylic acid methyl ester-1,1,1',1'-tetraoxide 3,4'-yl ethers 2a-d were synthesized through the oxidative dimerization of 7-substituted (or H)-4-hydroxy-2-alkyl-1,2-benzothiazine-3-carboxylic acid methyl ester 1,1-dioxides la-d using silver oxide($Ag_2O$). 4-Oxo-2,2'-dialkyl-1,1'2,2'-dibenzothiazine-3,3'-dicarboxylic acid methyl ester-1,1,1',l'-tetraoxide 3,4'-yl ether 2c was identified by X-ray crystal structure determination.

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Effect of ICT Capital on the Demands for Labor and Energy in Major Industries of Korea, US, and UK (ICT 자본 투입이 노동 및 에너지 수요에 미치는 영향: 한국, 미국, 영국의 제조업 및 전기·가스·수도사업의 생산구조 비교)

  • Kim, Jihyo;Heo, Eunnyeong
    • Environmental and Resource Economics Review
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    • v.23 no.1
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    • pp.91-132
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    • 2014
  • We investigate the effect of ICT capital on the demands for labor and energy in manufacturing and electricity gas water industries of Korea, US, and UK. Assuming ICT capital, non-ICT capital, labor, electricity, fuel, and material as input factors for manufacturing and ICT capital, non-ICT capital, labor and energy material as input factors for electricity gas water industry, we estimate the Morishima elasticities of substitution. Considering the relative price changes of input factors, ICT capital has substituted labor in manufacturing and electricity water gas industries of the three countries. ICT capital has substituted both electricity and fuel in US and UK manufacturing. Although ICT capital has substituted electricity and fuel each other in Korean manufacturing, ICT capital is unlikely to decrease the demands for electricity and fuel when considering their relative price changes. ICT capital has substituted energy material in electricity gas water industries of the three countries.

Kinetic Studies on Solvolyses of Substituted Cinnamoyl Chlorides in Alcohol-Water Mixture (알코올-물 혼합 용매계에서 치환된 염화신남오일의 가용매분해반응에 관한 속도론적 연구)

  • Koo, In Sun;Kim, Jung Soon;An, Sun Kyoung;Yang, Kyu Il;Lee, Ic Hoon
    • Journal of the Korean Chemical Society
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    • v.43 no.5
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    • pp.527-534
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    • 1999
  • Solvolyses of para-substituted cinnamoyl chlorides in aqueous binary mixtures of acetone, ethanol, methanol were investigated at 25.0$^{\circ}C$. These data were interpreted using the Grunwald-Winstein relationship, Hammett equation, and quantum mechanical model. Grunwald-Winstein plots of the first-order rate constants for para-substituted cinnamoyl chlorides with $Y_{CI}$ showed marked dispersions into three separate curves for the three aqueous mixtures with a large m vaIue for aqueous alcohol solvents. This study has shown that the potential energy surface and quanturm mechanical model predict transition state variation correctly for $S_N1$ like $S_N2$ reaction mechanism of para-substituted cinnamoyl chlorides.

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The Effects of Soy Protein Isolate on Quality and Acceptability of Soy Protein Isolate Substituted Beef Patties and Ice Cream (분리대두단백(分離大豆蛋白)의 Beef Patties와 아이스크림에 대(對)한 이용효과)

  • Kim, Chul-Jin;Byun, Si-Myung
    • Korean Journal of Food Science and Technology
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    • v.9 no.3
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    • pp.190-193
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    • 1977
  • In our previous report (Korean J. Food Sci. and Technol., 9, 123, 1977) we have studied the functional properties of soy protein isolates prepared from defatted soybean meal. For the practical application of the data described, beef patties substituted with SPI, and imitatied ice cream were prepared and sensory evaluations were carried out. The sensory analyses indicated that the beef patties substituted with gelated SPI to 30% have no detectable difference to the control at the significant level of 0.01. The imitation of ice cream whose milk-solid-not-fat was substituted with soy protein isolates showed the same texture as the control. Flavor of ice cream, however, has significant difference to the control due to beany-off flavor. Therefore removal of beany-off flavor is required for the substitution in ice cream.

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