• Title/Summary/Keyword: Substituted

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Synthesis, Spectral and Antimicrobial Studies of Some N(2)-Substituted Tetrahydroindazoles

  • Amirthaganesan, Shanmugasundaram;Aridoss, Gopalakrishnan;Park, Keun-Soo;Lim, Kwon-Taek;Jeong, Yeon-Tae
    • Bulletin of the Korean Chemical Society
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    • v.31 no.5
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    • pp.1135-1142
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    • 2010
  • A series of N(2)-benzothiazolyl substituted tetrahydroindazoles has been synthesized via cyclic ${\beta}$ keto esters. Optimum reaction condition was found as acidic toluene and effect of higher acidity towards substituted hydrazines in situ was described. Synthesized compounds have been achieved as single isomer and characterized by using 1D and 2D NMR spectral reports. Antimicrobial screening was carried out for the synthesized compounds along with a series of N(2)-pyridyl tetrahydroindazoles.1 The results of the in vitro antimicrobial screening studies revealed that compounds 13, 16 against Staphylococcus aureus, 11 against Escherichia coli, 10-12, 16 against Pseudomonas aeruginosa and 12 against Klebsiella pneumoniae recorded almost two-fold better activity compared to the standard drug used.

Synthesis of its Tautomeric Forms and New 6-Substituted Pyridazin-3(2H)-one Analogs (새로운 6-Substituted Pyridazin-3(2H)-one 유도체 및 토토머형의 합성)

  • Kim, Chaewon;Park, Myung-Sook
    • YAKHAK HOEJI
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    • v.57 no.5
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    • pp.316-322
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    • 2013
  • The new pyridazinone analogs were synthesized for development of candidates to retain anticancer activity. Various 6-substituted pyridazin-3(2H)-ones were prepared from the pyridazinyl chloride 3a~d via endothermic nucleophilic substitution with hydroxide ion as nucleophile for 2~48 h. Pyridazinyl chloride 3a~d could be converted to hydroxypyridazines (or pyridazin-3(2H)ones) using 1~5 equivalents of water (or 1 equivalent of sodium hydroxide) at reflux in DMF. The tautomerism of lactim form to lactam form was also accomplished in pyridazine derivatives. Formation of pyridazinones 10 was undertaken with stirring using sodium hydroxide at reflux in DMF for 2 h. Synthetic compounds were identified using NMR spectrum.

Electron Impact Ionization Mass Spectra of 3-Substituted-2-hydroxy-4(3H)-quinazolinones

  • El Deen, I.M.;Abd El Fattah, M.E.
    • Bulletin of the Korean Chemical Society
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    • v.24 no.4
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    • pp.473-478
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    • 2003
  • 3-Amino-2-hydroxy-4(3H)-quinazolinone (3) was prepared via condensation of 1 with hydrazine hydrate. Treatment of 3 with appropriate acid in $POCl_3$, ethyl chloroacetate and activated olefinic compounds in DMF yielded the corresponding 3-(substituted)amino-2-hydroxy-4(3H)-quinazolinones 4, 5 and 6. The electron impact ionization mass spectra of compounds 3 and 4 show a weak molecular ion peak and a base peak of m/z 146 resulting from a cleavage fragmentation. The compounds 5 and 6 give a characteristic fragmentation pattern with a very stable fragment of benzopyrazolone (m/z 132).

The Design and Synthesis of 1,4-Substituted Piperazine Derivatives as Triple Reuptake Inhibitors

  • Han, Min-Soo;Han, Young-Hue;Song, Chi-Man;Hahn, Hoh-Gyu
    • Bulletin of the Korean Chemical Society
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    • v.33 no.8
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    • pp.2597-2602
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    • 2012
  • Novel 1,4-substituted piperazine derivatives 5, Series A and B were designed by fragment analysis and molecular modification of 4 selected piperazine-containing compounds which possess antidepressant activity. We synthesized new 39 analogues of Series A and 10 compounds of Series B, respectively. The antidepressant screening against DA, NE, and serotonin neurotransmitter uptake inhibition was carried out using the Neurotransmitter Transporter Uptake Assay Kit. The compounds in Series B showed relatively higher reuptake inhibitory activity for SERT, NET, and DAT than those in Series A. The length of spacer between the central piperazine core and the terminal phenyl ring substituted at the piperazine ring in Series B seems to exert an important role in the activity.

Efficient Synthesis of Novel 3-Substituted Coumarin-3-carboxamide

  • Sheikhhosseini, Enayatollah;Balalaie, Saeed;Bigdeli, Mohammad Ali;Habibi, Azizollah;Moghaddam, Hamed Piri
    • Journal of the Korean Chemical Society
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    • v.58 no.2
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    • pp.186-192
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    • 2014
  • A series of novel pseudopeptides contained coumarin skeleton were synthesized through the Ugi-four-component reaction. The 3-substituted coumarin-3-carboxamides were formed through reaction of benzaldehyde derivatives, anilines, coumarin-3-carboxylic acid and isocyanides with high yields and high bond-forming efficiency at room temperature. These novel amidated coumarins exhibit brilliant fluorescence in range of 535-547 nm in chloroform.

Synthesis and Characterization of Substituted Quinoline Complexes of Molybdenum (I). Substituted Quinolinium Salts of Pentachlorooxomolybdate (V) (몰리브덴(V)의 퀴놀린계 착물합성과 그 성질 (제2보). 오클로로옥소몰리브덴(V) 산의 치환퀴놀린윰염)

  • Kwang Lee;Sang-Oh Oh
    • Journal of the Korean Chemical Society
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    • v.29 no.5
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    • pp.482-489
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    • 1985
  • The substituted quinolinium salts of pentachlorooxomolybdate (V) have been synthesized and characterized by means of the investigation of elemental analysis, infrared spectra, electron spectra, electric conductivity. The results of elemental analysis were well coincided with the theoretical value and all prepared salts were mononuclear complexes. The complexes were binary univalent electrolytes and analyzed d-d transition and charge transfer transition.

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Dielectric and Magnetic Properties of Niobium and Cobalt Co-substituted Multiferroic BiFeO3 Thin Films (Niobium과 Cobalt를 첨가한 Multiferroic BiFeO3 박막의 유전 특성 및 자성 특성)

  • Jun, Youn-Ki;Hong, Seong-Hyeon
    • Journal of the Korean Ceramic Society
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    • v.45 no.9
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    • pp.556-560
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    • 2008
  • The effects of Nb and Co ion substitution on the dielectric and magnetic properties of the multiferroic $BiFeO_3$ thin films have been investigated. Heteroepitaxial $BiFeO_3$ thin films were deposited by Pulsed Laser Deposition method. Nb substitution decreased the leakage current by 6 orders of magnitude and Co substituted $BiFeO_3$ thin films showed an enhanced magnetization, 2 times larger than that of un-substituted $BiFeO_3$. Through the co-substitution of Co and Nb, $BiFeO_3$ thin films with a low leakage current and an enhanced magnetization could be obtained.

Theoretical Studies on Substituent Effects of meta-Substituted Pyridines (메타 - 치환 피리딘의 치환기 효과에 대한 이론적 연구)

  • Lee, Gab-Yong;Song, Young-Dae
    • Journal of the Korean Chemical Society
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    • v.44 no.3
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    • pp.184-189
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    • 2000
  • ab initio molecular orbitaI calculation is performed to estimate the substituent effects for meta-substituted pyridines. Electrostatic potentials are obtained from ab initio wavefunctions of the optimized structures for the meta-substituted pyridines. Electrostatic potenhals are shown to be minimum at nitrogen atom of pyridines. The potenttial minima are good correlated with the substituent constants, ${\sigma}_m$ and with the ${\Delta}pK_a$, respectively. It is found that the electrostatic potential minima can be used as a useful measure of substituent effects.

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Synthesis and $\beta$-lactamase inhibitory activity of 6-exomethylene penamsulfone derivatives- I (Synthesis of 1-substituted thioalkyl -1,2,3-triazole-4-carboxaldehyde)

  • Yim, Chul-Bu;Youm, Jeong-Rok;Im, Chae-Uk;Park, Hee-Suk;Oh, Jeong-Suk;Park, Kye-Hwan
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1996.04a
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    • pp.159-159
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    • 1996
  • 6-Substituted exomethylene 기를 갖는 penam계 화합물이 $\beta$-lactamase 억제제로서 강력한 활성을 보여주고 있어서, 6-exomethylene기 도입에 필요한 1-substituted thioalkyl-1,2,3-triazole-4-carboxaldehyde를 합성하였다. Haloalkanol에 NaN$_3$를 반응시켜서 합성한 azidoalkanol과 propargyl alcohol을 산화시킨 propargyl aldehyde를 반응시켜서 1-(2-hydroxyalkyl-1,2,3-triazole-4-carboxaldehyde을 얻었다. 이것을 trifluoromethanesulfonic anhydride와 triethylamine 존재 하에 mercapto 화합물과 반응시켜서 목적물을 합성하였다.

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Physicochemcal Properties of Jeungpyun, Korean Traditional Fermented Rice Cake Prepared with Brown Rice and Barley Flour

  • Hye Young L. Kim;Mie Ja Park
    • Korean Journal of Environmental Biology
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    • v.21 no.4
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    • pp.377-383
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    • 2003
  • The functional Jeungpyuns with dietary fiber containing cereals such as brown rice and barley flour were developed and physiochemical properties were investigated. The water binding capacity had significantly the highest value of 28.4% in raw rice flour, followed by brown rice flour and barley flour. The lowest reducing sugar value was seen in unpolished rice substituted Jeungpyun with value of 5.420 (P<0.05). The amount of reducing sugar decreased slightly after steaming, due to the increased degree of sugar dissociation. The L value of the lightness decreased significantly with the substituted samples (P< 0.05). The barley substituted samples were darker than that of brown rice sample groups with less green and yellow color. Microstructures of starch particles after fermentation showed completely dispersed starch particles with air bubbles and sponge-like structure in all samples after steaming. Thus, functional Jeungpyun replaced with brown rice and barley flour can be successfully formulated and has been influenced by the physicochemical properties.