• Title/Summary/Keyword: 1-dioxide derivatives

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Studies on the Synthesis of 3-oxo-1, 2-benzisothiazole-1, 1-dioxide Derivatives and their Antifungal Activity against Pyricularia oryzae (3-Oxo-1, 2-benzisothiazole-1, 1-dioxide 유도체들의 합성 및 Pyricularia oryzae에 대한 항균성에 관한 연구)

  • Yoon, Yong-Jin;Choi, Sam-Young;Park, Chang-Suk;Lee, Chong-Kwang
    • Applied Biological Chemistry
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    • v.29 no.2
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    • pp.164-174
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    • 1986
  • 도열병균에 의한 벼의 목 및 잎도열병에 효과가 좋은 새로운 살균제의 개발을 시도하였다. 농약으로 예상되는 몇몇 3-oxo-1, 2-benzisothiazole-1, 1-dioxide의 새로운 유도체들을 합성하고, 이들 유도체들의 도열병균 (Pyricularia oryzae)에 대한 항균성을 agar medium dilution 방법에 의해 측정하였다. 3-oxo-1, 2-benzisothiazole-1, 1-dioxide의 5 원자 고리의 3개 구조 단위중에서 가장 항균성이 큰 단위는 $R-S-C=N-SO_2-$단위이며, 3개 구조 단위의 항균성 순서는 $RS-C=N-SO_2-\;{\geq}\;RO-C=N-SO_2-\;>\;-CNR-SO_2-$였다. 30개 후보화합물 가운데서 14개의 유도체가 도열병균에 효능이 좋은 것으로 알려진 oryzemate 보다 우수한 항균성을 나타냈다.

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The Synthesis of 1,2-Benzothiazine-3-carboxamidylhydantoin Derivatives and their Antiinflammatory and Analgesic Activities

  • Kwon, Sonn-Kyoung;Park, Myoung-Suk
    • Archives of Pharmacal Research
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    • v.15 no.3
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    • pp.251-255
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    • 1992
  • A number of 4-hydroxy-2H (or alkyl)-N-(3-aralkyl-2-thio-1-hydantoinyl)-1, 2-benzothiazine3-carboxamide 1, 1-dioxides were synthesized through the reaction of 4-hydroxy-2H (or alkyl)1, 2-benzothiazine-3-carboxylic methyl ester 1, 1-dioxide and 1-amino-2-thio-3-aralkyl-4-imidazolones in xylene. The compounds synthesized were screened for antinflammatory effect on carrageenin-induced edema in rat and for analgesic effect on acetic acid-induced Writhing syndrome in mice. Most compounds were inhibots of carrageenin-induced rat foot edema and some showed significant antinflammatory activity comparable to that of indomethacin and significant analgesic activity comparable to that of indomethacin and aspirin.

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Studies on Isoindoline Derivatives. III. Studies on the Anhydrides and Imides of Dibasic Acids for the Organic Acids in the Gabriel Condensation (Isoindoline 유도체의 합성연구 III 이염기산무수물 또는 Imjde에 대한 유기산의 Gabriel 축합반응에 관한 연구)

  • 이남순;임중기;조태순;원정희;문도원;박인석;김무곤;민윤식;정진수
    • YAKHAK HOEJI
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    • v.18 no.1
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    • pp.59-73
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    • 1974
  • Fifteen derivatives of phthalide were synthesized from m-hemipinic, hydrastic and 4,5-benzophthalic anhydride with acetic, phenylacetic, p-methoxyphenylacetic, p-nitrophenylacetic, ${\alpha}$-nephthylacetic and succinic acid by the Gabriel condensation. In the same way, 13 derivatives of phthalimidine and 4 derivatives of ${\alpha,\beta}$ -benzisothiazoline-1, 1-dioxide were synthesized from diphenylmaleimide, phthalimide, saccharine and 4,5-benzo-phthalimide with previous 6 acids. 3-Substituted derivatives of m-hemipinic anhydride, hydrastic anhydride and 4,5-benzophthalic anhydride were treated with formamide and seven 3-substituted imidines could be synthesized. In case of 4,5-benzophtha lide, two isomers,4,5-benzophthalidene-3-acetic acid and 4,5-benzophthalidene-1-acetic acid, can be obtained theoretically, but only one product we got, and the chemical structure of it was identified by the following way. It was hydrolyzed and then decarboxylated, and this decomposed product was identical with 1-acetyl-2-naphthoic acid which was synthesized from .betha.-naphthylamine. This indicates that by the Gabriel condensatioin 4,5-benzophthalide only produces 4,5-benzophthlidene-3-acetic acid, that is ${\alpha}$-carbonyl substitute.

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Software approach towards understanding meteorological data for environmental monitoring and assessment of peninsular Malaysia

  • Quadri, Sayed Abulhasan;Sidek, Othman;Jafar, Hadi;binti Amran, Nur Amira;bt Zabah, Ummi Nurulhaiza;bin Abdullah, Azizul
    • Advances in environmental research
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    • v.3 no.1
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    • pp.87-106
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    • 2014
  • The concern for the global environment ensues researchers from various disciplines to work in collaboration to tackle with the issues of sustainability and environmental conservation for well-being of the people. In this study, we have selected and focused on few basic environment-effecting factors such as temperature, humidity, carbon dioxide and oxygen concentration level and referred them as meteorological data. In this paper, we present the development of our own customized hardware setup, environmental monitoring device (EMD) to obtain the data. Utilizing the relationship among these basic parameters, represented in the form of formulas and equations, we tried to encode them using Matlab programming. Data visualization is achieved by plotting the graphs of basic parameters obtained from EMD as well for the derivatives using Matlab programs.

Synthesis and Cytotoxicity of Some Rigid Derivatives of Methyl 2,5-Dihydroxycinnamate

  • Nam, Nguyen-Hai;Kim, Yong;You, Young-Jae;Hong, Dong-Ho;Kim, Hwan-Mook;Ahn, Byung-Zun
    • Archives of Pharmacal Research
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    • v.25 no.5
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    • pp.590-599
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    • 2002
  • Eight rigid compounds designed as esterase-stable analogues of methyl 2,5-dihydroxycinnamate (1) were synthesized. These derivatives include 2-(2',5'-dihydroxybenzylidene)cyclopentenone (3a), 2-(2',5'-dihydroxybenzylidene)cyclohexanone (3b), 2,6-bis(2',5'-dihydroxybenzy-lidene)cyclohexanone (4b), 2,6-bis(2',5'-dihydroxybenzylidene)cyclopentenone (4a), (E)-3-(2',5'-dihydroxybenzylidene)pyrrolidin-2-one (5), (E)-5-(2',5'-dihydroxybenzylidene )-1,2-isothiazolidine-1,1-dioxide (6), 4-(2',5'-dihydroxyphenyl)-5H-furan-2-one (7), and 3-(2',5'-dihydroxyphenyl)cyclopent-2-ene-1-one (8). Among the eight compounds, the furanone 7 and cyclopentenone 8 showed the most potent cytotoxicity with $IC_{50}$ values of 0.39-0.98 $\mu\textrm{g}$/mL. Compound 8 was further brominated, phenylated and methylated at the a position to give three corresponding analogues, including 2-bromo-3-(2',5'-dihydroxyphenyl)cyclopent-2-ene-1-one (24), 3-(2',5'-dihydroxyphenyl)-2-phenylcyclopent-2-ene-1-one (27), and 3-(2',5'-dihydroxyphenyl)-2-methylcyclopent-2-ene-1-one (28). Among the three, the most enhanced activity was observed with the phenylated compound 27.

Studies on Synthesis of 1,2- and 1,3-Diamine Derivatives: Synthesis and Molecular Structure of 3-(N-Benzylamino)-4,5-dihydro-1,2,5-thiadiazole 1,1-dioxides (1,2- 그리고 1,3-디아민 유도체의 합성에 관한 연구(Ⅰ): 3-(N-벤질아미노)-4,4-디히드로-1,2,5-티아디아졸 1,1-디옥시드의 합성과 분자구조)

  • Lee, Chai-Ho;Kim, Eui-Sung;Chung, Bong-Young;Lee, Yeong-Haeng
    • Journal of the Korean Chemical Society
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    • v.40 no.7
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    • pp.526-530
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    • 1996
  • 3-(N-Alkylamino)-4,5-dihydro-1,2,5-thiadiazole 1,1-dioxides have been prepared by the treatment of 3-imino-1,2,5-thiadiazolidine 1,1-dioxides with alkylamines. The selected spectral properties of these heterocycles are detailed, as well as an X-ray crystallographic structure of a representative member of these compounds. 3-(N-Benzylamino)-4,5-dihydro-4-(4'-methoxyphenyl)-1,2,5-thiadiazole 1,1-dioxide crystallyzes in space group $P2_1a$, monoclinic, with $a=22.512(3)(1)\AA$, $b=9.831(2)\AA$, $c=7.194(4)\AA$, $\beta=96.65(2)$, and Z=4.

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Synthesis of Novel 1,2-Diazepino[3,4-b]quinoxaline and Pyridazino[3,4-b]quinoxaline Derivatives (새로운 1,2-Diazepino[3,4-b]quinoxaline과 Pyridazino[3,4-b]quinoxaline)

  • Kim, Ho Sik;Jeong, Geuk
    • Journal of the Korean Chemical Society
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    • v.43 no.3
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    • pp.302-306
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    • 1999
  • The 1,3-dipolar cycloaddition reaction of the quinoxaline 4-oxide 10 with 2-chloroacrylonitrile gave the 2,3-dihydro-lH-1,2-diazepino[3,4-blquinoxalines lla, b, respectively, which were converted into the 2,3,4,6-tetrahydro-lH-l,2-diazepino[3,4-b]quinoxaline 12. The reaction of compound lla with selenium dioxide in acetic acid/water resulted in ring transformation to give the 1,4-dihydro-4-oxopyridazino[3,4-blquinoxaline 13.

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Prediction of Phase Behavior of ε-caprolactam Derivatives and Carbon Dioxide using a Group Contribution Method (그룹 기여 방법을 이용한 ε-caprolactam 유도체와 이산화탄소의 상거동 예측에 관한 연구)

  • Kwon, Soyoung;Bae, Won;Lee, Kyoungwon;Kim, Hwayong
    • Clean Technology
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    • v.11 no.3
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    • pp.117-122
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    • 2005
  • N-vinyl caprolactam (NVCL), a kind of N-vinyl amide monomer, must be dissolved in continuous phase ($scCO_2$) for dispersion polymerization in supercritical carbon dioxide. Phase behavior of $CO_2$+NVCL is very important and necessary for determining initial polymerization condition and for monomer extraction from final polymer. There is the limitation of experimental method for obtaining pure properties of the monomer because of the possibility of polymerization. And N-methyl caprolactam (NMCL) is the useful solvent for the gas treating process. In the viewpoint of molecular thermodynamics, NVCL and NMCL have same functional group i.e. ${\varepsilon}$-caprolactam. In the case of NVCL, hydrogen of amide group is substituted with vinyl group and for NMCL, hydrogen of amide group is substituted with methyl group. We suggested modified group contribution method for this ${\varepsilon}$-caprolactam derivatives. This new group contribution parameter was applied to correlate $CO_2$ + N-vinyl caprolactam or N-methyl caprolactam system.

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