• Title/Summary/Keyword: Alkyl-3

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Comparative Molecular Field Analyses (CoMFA) on the Mela-nogenesis Inhibitory Activities of Alkyl-3,4-dihydroxybenzoyl Derivatives.

  • Kim, Sang-Jin;Sung, Nack-Do;Lee, Tack-Hyuck
    • Proceedings of the SCSK Conference
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    • 2003.09a
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    • pp.225-231
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    • 2003
  • To search and development a new material with superior melanogenesis inhibitory activity, the bioactivities (obs. pl$_{50}$) of alkyl-3,4-dihydroxybenzoyl esters and N-alkyl-3,4-dihydroxybenz-oyl amides as substrate molecules were measured in mouse melanoma cells. And also, we have studied that 3-D QSARs (3 dimensional Quantitative Structure-Activity Relationships) between molecular interaction field of substrates and the bioactivities were analyzed using CoMFA (Comparative Molecular Field Analyses) method. When cross-validation value (q$^2$) is 0.68 at 3 components, the Pearson correlation coefficient ($r^2$) is 0.900. From the basis on the findings, the model was appeared by the contour map such as steric field and electrostatic field relationships between quantitative structure and the bioactivity of the various substrate derivatives. Measured bioactivities (obs. pl$_{50}$) of unknown compounds are very similar to predicted activity (pred. pl$_{50}$) according to the CoMFA model. As the results of prediction, we could conclude that the bioactivities were increased by creation of R$_1$ substitution of 5,5-dime-thylhexoxy, 6,6-dimethylheptyl, 1-amino-6,6-dimethylheptyl group etc and R$_2$ substitution of hydroxy, methyl, methoxy group etc.p etc.

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The Synthesis of 6-Fluoroquinolone Carboxamidopenicillin Derivatives (6-Fluoroquinolone Carboxamidopenicillin 유도체의 합성)

  • 임철부;김정주
    • YAKHAK HOEJI
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    • v.31 no.2
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    • pp.92-97
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    • 1987
  • The N-[1H-6-fluoro-1,4-dihydro-4-oxo-7-chloroquinoline-3-carboxy] succinimide was reacted with amoxicillin, ampicillin and 6-APA to give 6-[D-(-)-$\alpha$-{1H-6-fluoro-1,4-dihydro-4-oxo-7-chloroguinoline-3-carboxamido} p-hydroxyphanyl acetamido] penicillanic acid [1], 6-[D-(-)-$\alpha$-{1H-6-fluoro-1,4-dihydro-4-oxo-7-chloroquinoline-3-carboxamido} phenylacetamido] penicillanic acid [10] and 6-[1H-6-fluoro-1,4-dihydro-4-oxo-7-chloroquinoline-3-carboxamido] penicillanic acid [19]. The 1-alkyl-6-fluoro-1,4-dihydro-4-oxo-7-substituted quinoline-3-carboxylic acids were reacted with ethyl chloroformate for making mixed anhydride; these mixed anhydrides were reacted with amoxicillin, ampilcillin and 6-APA to give 6-[D-(-)-$\alpha$-{1-alkyl-6-fluoro-1,4-dihydro-4-oxo-7-substituted quinoline-3-carboxamido} p-hydroxyphenylacetamido] penicillanic acid [2-9], 6-[D-(1)-$\alpha$-{1-alkyl-6-fluoro-1,4-dihydro-4-oxo-7-substituted quinoline-3-carboxamido} phenylacetamidod penicillanic acid [11-18] and 6-[1-alkyl-6-fluoro-1,4-dihydro-4-oxo-7-substituted quinoline-3-carboxamido] penicillanic acid [20-27].

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Synthesis of 1N-alkyl-2-amino-3-ethoxycarbonyl-pyridino [2,3-f]indole-4,9-dione derivatives (I) (1N-알킬-2-아미노-3-에톡시카르보닐-피리디노 [2,3-f]인돌-4,9-디온 유도체의 합성 (I))

  • Suh, Myung-Eun;Shin, Sung-Hee
    • YAKHAK HOEJI
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    • v.41 no.5
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    • pp.575-581
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    • 1997
  • The 6,7-dichlorquinoline-5,8-dione was reacted with ${alpha}$-cyanoacetic acid ethyl ester in ammonia solution to yield 6-(${alpha}$-cyano-${alpha}$-ethoxycarbonyhnethyl)-7-chloroquinoline- 5,8-dione (compound I). When this compound was reacted with some alkyl amines (methylamine, ethylamine, isopropylamine, etc) 2-amino-3-ethoxycarbonyl-N-alkyl-pyridino[2,3-f]indole-4,9-diones (compounds II a-e) were obtained.

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Synthesis of 1,4-Bis(1'-alkyl-2',3',4',5'-tetraphenyl-1'-silacyclopentadienyl)benzenes (1,4-Bis(silyl)benzene의 고리화반응에 의한 1,4-Bis(1'-alkyl-2',3',4',5'-tetraphenyl-1'-silacyclopentadienyl)benzenes 리간드의 합성)

  • Kong, Young Kun;Ahn, Young Man
    • Journal of the Korean Chemical Society
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    • v.41 no.2
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    • pp.82-87
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    • 1997
  • The 1,4-bis(alkyldichlorosilyl)benzene was synthesized to be a precursor of the bis(silacyclopentadienyl) aromatic system. The cyclization reaction of the precursor with 1,4-dilithio-1,2,3,4-tetraphenyl-1,3-butadiene produced the 1,4-bis(1'-alkyl-2',3',4',5'-tetraphenyl-1'-silacyclopentadienyl)benzene as the ligand of organotransition metal compound and the precursor of the stable silacyclopentadienyl anion.

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PHOTOCHEMICAL REACTIONS OF PSEUDOSACCHARIN 3-ALLYL ETHER (PROBENAZOLE) AND ITS ALKYL ETHER

  • Yoon, Ung-Chan
    • Journal of Photoscience
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    • v.2 no.2
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    • pp.77-81
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    • 1995
  • Photoreactions of pseudosaccharin ethers have been investigated. Pseudosaccharin 3-allyl ether undergoes a facile photoreaction via reaction pathways involving homolysis of bond between pseudosaccharyl oxygen and 3-allyl carbon, and excited nucleophilic substitution of allyloxy group by solvent which are not quenched by oxygen present in the reaction. Product yield demonstrates that the homolysis pathway predominates over the nucleophilic substitution in ca. 7:1 ratio. In contrast, pseudosaccharin alkyl ethers follow different reaction routes to produce two products, solvent-substituted pseudosaccharin alkyl ethers and reduction products, 3-alkoxy-1, 2-benzisothiazoles. The formations of reduction products, 3-alkoxy-1, 2-benzisothiazoles are completely quenched by oxygen.

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Electrochemical Behaviors for Cathodic Reaction of N'-aryl-N-alkyl-N-nitrosourea Drivatives (N'-aryl-N-alkyl-N-nitrosourea 유도체의 환원반응에 대한 전기화학적 거동)

  • Won, Mi Sook;Kim, Jack C.;Jeong, Euh Duck;Shim, Yoon-Bo
    • Journal of the Korean Chemical Society
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    • v.39 no.11
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    • pp.842-847
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    • 1995
  • The electrochemical reduction reactions of N '-aryl-N-alkyl-N-nitrosourea derivatives with a glassy carbon electrode were diffusion controlled and irreversible. The exchange kinetic constant ko values for reduction reaction of the N '-aryl-N-alkyl-N-nitrosoureas were at the range of $1.48{\times}10^{-6}{\sim}5.32{\times}10^{-7}\;cm/sec.$ The $k_0$ values for phenyl substituted on the aryl position were about 1.3∼2.8 times higher than that of other substituents. The same substituent for aryl groups on the both of N '-aryl-N-alkyl-N-nitrosourea and N '-aryl-N-(2-chloroethyl)-N-nitrosourea exhibited same value. The $E_p$ value was shifted to the negative direction as pH increased. The number of protons participated to the reduction was 4∼5, respectively. The substituent effect of aryl group on the reduction potential was not observed in this case.

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Optical and Electronic Properties of Polyalkylthiophene (폴리알킬시오펜의 전자 및 흡광특성)

  • 박대희
    • Electrical & Electronic Materials
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    • v.10 no.8
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    • pp.778-782
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    • 1997
  • In this paper the electronic and optical properties of various poly(3-alkylthiophene)s differing in alkyl chain length were investigated. And their dependence on temperature were also investigated. The electrical conductivity decreased with the increase of alkyl chain length. In addition optical properties were changed due to the shift of edge energy which was caused by the change of the alkyl chain length and rise of temperature. The conformational change of poly(3-alkylthionphene) depending on the alkyl chain length is believed to be responsible to the change of electronic and optical properties of materials.

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The Identification of Spilled Oil by the Pattern of Alkyl PAH

  • Bae, Il-Sang;Shin, Ho-Sang;Lee, Jae-Young;Jung, Kweon;Lee, Yeon-soo
    • Proceedings of the Korean Society of Soil and Groundwater Environment Conference
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    • 2004.04a
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    • pp.289-292
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    • 2004
  • In order to identify the origin and nature of the spilled oil in the potential source, we analyzed the pattern of alkyi PAM(Polynuclear Aromatic Hydrocarbons) in fuel standard and environmental samples. Alkyl PAM patterns are used for fuel-type identification in weathered environmental samples. Detection of alkyl PAH was achieved by operation CC/MS in the SIM mode. We chose ions of naphthalene(m/z 128), C1-naphthalene(m/z 142), C2-naphthalene(m/z 156), C3-naphthalene(m/z 170), C4-naphthalene(m/z 184) for the comparison of this pattern according to the type of fuel. We analyzed tile pattern of alkyl PAH in neat gasoline, kerosene, diesel, and JP-8, and in groundwater samples which were collected in monitoring wells. The distribution map of alkyl-naphthalene shows different patterns among four different fuel types (gasoline, kerosene, diesel, and JP-8). Particularly, tile distribution map of kerosene and JP-8 is found to be of value in identifying fuel type in that the difference is clear. Therefore distribution patterns of alkyl-PAH compounds provide another useful tool for fuel-type identification of petroleum fuels.

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Studies on Physical Behavior of Alkyl Polyglucosides (I) - Interfacial Activities and Detergency - (Alkyl Polyglucoside 계면활성제의 물리적 거동에 관한 연구 (I) - 계면활성과 세정력에 관하여 -)

  • Yoon, Yeo-Kyung;Choi, Kyu-Suk
    • Applied Chemistry for Engineering
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    • v.5 no.3
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    • pp.451-456
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    • 1994
  • Alkyl polyglucosides (APG), so called natural nonionic surfactants, are prepared with glucose from corn starch and fatty alcohol from palm and/or coconut oil. When we studied on interfacial properties of APG, surface and interfacial tension, cmc, foaming and effectiveness, according to degree of polymerization of glucose unit (D.P.=1.2~1.8) and alkyl chain length, the former hardly affects but the latter greatly affects on them. The order of detergency for fatty acid soils decreased as followings ; APG 0814> APG 1214> APG 10> APG 0810> APG 08, and the samples with lowest interfacial tension and maximum adsorption had a better detergency.

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Synthesis and Antimicrobial Activity of Some New 1-Alkyl-2-alkylthio-1,2,4-triazolobenzimidazole Derivatives

  • Mohamed, Bahaa Gamal;Hussein, Mostafa Ahmed;Abdel-Alim, Abdel-Alim Mohamed;Hashem, Mohammed
    • Archives of Pharmacal Research
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    • v.29 no.1
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    • pp.26-33
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    • 2006
  • Some new derivatives of 1,2,4-triazolo[2,3-a]benzimidazoles were synthesized through the reaction of 1,2-diaminobenzimidazole with carbon disulfide. The resulting 1,2,4-triazolo-[2,3a]benzimidazole-2-thione intermediate was reacted with one equivalent of alkyl halides to give the corresponding 2-alkylthio derivatives, which were further alkylated through the reaction with another one equivalent of different alkyl halides to afford the target compounds; 1-alkyl-2alkylthio-1,2,4-traizolo[2,3-a]benzimidazoles. On the other hand, the 1,2-disubstituted derivatives with two identical alkyl substituents were prepared by the reaction of 1,2,4-triazolo[2,3-a]benzimidazole-2-thione with two equivalents of the alkyl halides. The structures of the new compounds were assigned by spectral and elemental methods of analyses. The synthesized compounds were tested for their antibacterial and antifungal activities. Most of the tested compounds proved comparable results with those of ampicillin and fluconazole reference drugs. The study indicated that, the antibacterial as well as the antifungal activities of the test compounds were improved with increase in the bulkiness of the introduced alkyl groups. Also, some active antibacterial compounds were tested for their antimycobacterial activity. All the test compounds showed equipotent antitubercular activity as that of INH as a reference drug.