• Title/Summary/Keyword: 6-dihydro-1

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Joint Toxic Action of Carbofuran and Diazinon Mixture Against the Larvae of the Common Cutworm (Agrotis fucosa Butler) (거세미나방 유충에 대한 $Carbofuran{\cdot}Diazinon$혼합의 연합독작용)

  • Ahn Y.J.;Kim Y.T.;Kim H.J.;Choi S.Y.
    • Korean journal of applied entomology
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    • v.19 no.2 s.43
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    • pp.73-78
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    • 1980
  • Some experiment were conducted to evaluate the joint toxic action of carbofuran(2,3-Dihydro-2, 2-dimethyl-benzofuranyl methyl carbamate) and diazinon (0.0-Diethyl-0-(2-isopropyl-6-methyl-e-pyrimidinyl)-0-thionophosphate) against 3rd-instar larvae of the common cutworm, Agrotis fucosa (Butler). Acetone solutions of carbofuran or diazinon or mixture of these two insecticides, were topically applied to the mesonotum of the insect in a constant volume of $1.0{\mu}l$ per larva by means of Burkard microapplicator. Joint toxic action of carbofuran and diazinon for 3rd-instar larva of common cutworm was synergistic. The maximum synergistic effect might be obtained when the ratio of carbofuran to diazinon was 4.8 : 5.2.

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A Solid Phase Synthesis of Dihydro-1,4-dioxin and Dihydro-1,4-oxathiin Carboxanilides Using Polymer-bound Oxime Ester (고체상에 연결된 옥심 에스테르를 이용한 다이하이드로-1,4-다이옥신 및 다이하이드로-1,4-옥사티인 카르복스아닐라이드 유도체의 고체상 합성)

  • Hahn, Hoh-Gyu;Bae, Su-Yeal;Nam, Kee-Dal
    • The Korean Journal of Pesticide Science
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    • v.10 no.1
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    • pp.1-6
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    • 2006
  • A methodology for the syntheses of carboxanilides using solid support of 4-chloro-3-nitorbenzophenone oxime resin 5 was developed. Condensation of 4-chloro-3-nitorbenzophenone resin 6 with hydroxylamine hydrochloride salt gave oxime resin 5. The reaction of oxime resin 5 with dioxin and oxathiin derivatives 7a-d afforded the corresponding polymer-bound dioxin and oxathiin derivatives 9a-d. These polymer-bound resins 9a-d were treated respectively with aniline in the presence of acetic acid resulted in the corresponding dioxin carboxanilides 10a-d (yield, 5%-quantitative).

Studies on the Synthesis of Pterdine Substituted Pyridonecarboxylic Acids as Potential Antibacterial Agents and their Antimicrobial Activities (항균제로서 Pteridine이 치환된 Pyridonecarboxylic Acids의 합성 및 항균 작용에 관한 연구)

  • Ryu, Seoung Ryuall;Choo, Dong Joon
    • Applied Chemistry for Engineering
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    • v.7 no.6
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    • pp.1096-1104
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    • 1996
  • In order to synthesize a new antibacterial and antitumor agents, we have prepared new analogues pteroic acid(13a, 13b), which means C-9 position of pteroic acid has been replaced by norfloxacin(8) or ciprofloxacin(9) and amino group of C-2 position by $CH_3$. These derivatives were synthesized coupling at N-4 piperazine of norfloxacin and ciprofloxacin with 2-amino-3-cyano-5-chloromethylpyrazine(20) provided 1-alkyl(ethyl, cyclopropyl)-6-fluoro-1,4-dihydro-4-oxo-7-[[4-N-(2-amino-3-cyanopyrazin-5-yl)methyl]piperazin-1-yl]-3-quinoline-carboxylic acid(12a, 12b). It was then cyclized with acetamidine. HCI to obtain new analogues of C-2 desaminomethylpteroic acid(13a, 13b) in yield of 76.2% and 82.8 % respectively. These compounds were tested in vitro on antibacterial activity against Gram-positive and Gram-negative bacteria including Pseudomonas aeruginosa ATCC9027. In general, these synthesized compounds(13a, 13b) showed less potent activities than those of norfloxacin.

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Attempted Synthesis of Carboxin Derivative through Ring Expansion Reaction on Solid Phase (고체상에서 환팽창 반응에 의한 카르복신 유도체의 합성시도)

  • Hahn, Hoh-Gyu;Bae, Su-Yeal;Nam, Kee-Dal
    • The Korean Journal of Pesticide Science
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    • v.9 no.3
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    • pp.185-190
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    • 2005
  • Solid phase synthesis of 16, which is a derivative of the first systemic fungicide, carboxin 1 was described. Reaction of 1,3-oxathiolane derivative with solid resin of 4-hydroxy-3-nitrobenzophenone 6 gave 9 in 82% yield. Oxidation of sulfur in the solid 1,3-oxathiolane 9 by MCPBA followed by a ring expansion reaction under the acid catalyst afforded the corresponding dihydro-1,4-oxathiin derivative 12. Treatment of the solid 1,3-oxathiolane 9 with p-methoxyaniline resulted in 1,3-oxathiolane 14, 1,3-oxathiolane sulfoxide 15, dihydro-1,4-oxathiin 16, and acetoacetanilide derivative 17 in 41%, 35%, 14%, 10% yields, respectively.

Isolation and Identification of the Antioxidant DDMP from Heated Pear (Pyrus pyrifolia Nakai)

  • Hwang, In Guk;Kim, Hyun Young;Woo, Koan Sik;Lee, Sang Hoon;Lee, Junsoo;Jeong, Heon Sang
    • Preventive Nutrition and Food Science
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    • v.18 no.1
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    • pp.76-79
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    • 2013
  • We evaluated antioxidant activities of heated pear juice (HPJ) exposed to 120, 130, and $140^{\circ}C$ for 2 hr. HPJ was partitioned using n-hexane, chloroform, ethyl acetate, n-butanol, and water. The ethyl acetate fraction treated at $130^{\circ}C$ for 2 hr showed strong antioxidant activity; thus, this extract was isolated and purified using silica gel column chromatography and preparative high performance liquid chromatography. The structure of the purified compound was determined using ultraviolet and mass spectrometry, $^1H$-nucelar magnetic resonance (NMR), and $^{13}C$-NMR. Antioxidant activities of the isolated compound were evaluated and compared with ${\alpha}$-tocopherol, ascorbic acid, and butylated hydroxytoluene (BHT) using DPPH and ABTS assays. The isolated compound was identified as 2,3-dihydro-3,5-dihydroxy-6-methyl-4H-pyran-4-one (DDMP). The DPPH radical-scavenging activity ($IC_{50}$) of DDMP occurred in the following order: ascorbic acid ($45.3{\mu}g/mL$) > ${\alpha}$-tocopherol ($69.2{\mu}g/mL$) > DDMP ($241.6{\mu}g/mL$) > BHT ($268.0{\mu}g/mL$). Furthermore, DDMP showed strong ABTS radical-scavenging activity (569.0 mg AA eq/g).

Cyclocondensation of 2-Substituted-4-hydroxy-2H-1, 2-benzothiazine-3-carboxylic acid 1, 1-dioxides with Dicyclohexylcarbodiimide (2-치환 4-Hydroxy-2H-1, 2-benzothiazine-3-carboxylic acid 1, 1-dioxidies와 Dicyclohexylcarbodiimide의 축합환화 반응)

  • 서정진;홍유화
    • YAKHAK HOEJI
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    • v.31 no.1
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    • pp.40-41
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    • 1987
  • 4-Hydroxy-2H-1, 2-benzothiazine-3-carboxylic acid 1a was reacted with 2 equivalents of dicyclohexylcarbodiimide (DCC) to give 2-cyclohexyl-3-cyclohexylimino-4,5-dihydro-1H-imidazo [1,5-b][1,2] benzothiazine-10, 10a-dyhydro-1,10-dione 5,5-dioxide 2a and dicyclohexylurea (DCU). On the other hand 2-substituted-4-hydroxy-2H-1, 2-benzothiazine-3-carboxylic acid 1,1-dioxide 1b or c was reacted with DCC to give 2-cyclohexylimino-3-cyclohexyl-5-alkyl-4-oxo-2,5H-1,3-oxazino [5,6-c]-1,2-benzothiazine 6,6-dioxide 2b or c and DCU.

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Volatile Flavor Components of Soybean Paste(Doenjang) Prepared from Different Types of Strains (균주를 달리한 된장의 향기 성분)

  • Park, Jung-Suk;Lee, Myung-Yul;Kim, Kyong-Su;Lee, Taik-Soo
    • Korean Journal of Food Science and Technology
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    • v.26 no.3
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    • pp.255-260
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    • 1994
  • Four types of soybean paste(Doenjang), using traditional meju, koji, natto meju and mixture of koji and natto meju, were manufactured and fermented for 90 days. Analyzed volatile flavor components by GC-MS were confirmed to be thirty-six components including 5 alcohols, 5 aldehydes. 8 ketones, 3 acids, 9 esters and 6 miscellaneous ones. Traditional soybean paste tested had 29 components, koji and koji-natto soybean paste $26{\sim}24$ and natto soybean paste had 20 ones. Alcohol was found to be the most abundant volatile flavor components in all samples group. Traditional soybean paste had higher ratio of carbonyl to ester than any other types of soybean paste while koji-natto soybean paste had the lowest ratio of their components. The newly identified five volatile flavor components were 3-ethoxy-l-propene, dihydro-2-methyl-3-furanone. 1-hydroxy-2-propanone, 1-(2-furanyl)ethanone and 2-acethyl ethylhexanoate.

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Synthesis of Pyrazolo [4,3-c]Pyridazine and Isoxazolo [3,4-d]Pyridazine Derivatives

  • Abbass, Ikhlass-M.;Sharaf, Mohye-A.F.;El-damaty, Alia-A.
    • Archives of Pharmacal Research
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    • v.16 no.2
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    • pp.164-167
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    • 1993
  • Arylhydrazones of diethyl acetonedicarboxylate 3 was treated with fomaldehyde to 1-aryl-1, 4, 5, 6-tetrahyeheypyridazine derivatives 4a-f Cyclization of compound 4a-f by hydroxy-lamine afforded [3, 4-d] 1, 4, 5, 6-tetrahydropyridazine derivative 5a-f. Also, cyclization of compound 4c with semicarbazide gave pyrazolote [4, 3-c] pyridazine 6. On the other hand compound 3 reacted with ethylothofomate to give diethyl-1, 4-dihydro-1-arypyridazine-4-one-3, 5 dicaboxylate 7, which on treatment with hydrazine, semicarbazide and thiosemicarbazide gave pyridazine, amido and thioamido derivatives. The spectrl and antimicrobial data of these compounds 1-8 were studied.

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The Determination of Enoxacin with p-Quinone Derivatives (파라퀴논 유도체와의 전하이동착물 형성을 이용한 에녹사신 정량)

  • 이지연;김동오;남수자;정문모;허문회;안문규
    • YAKHAK HOEJI
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    • v.43 no.4
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    • pp.437-441
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    • 1999
  • Enoxacin[1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-\piperazinyl)-1,8-naphthyridine-3-carboxylic acid, ENX] is a new quinolone antibacterial agent. The method is based on the highly colored charge-transfer complex formation of this drug as a $\pi$-electron donor with 7,7,8,8-tetracyanoquinodimethane(TCNQ) or chloranil(CL) as $\pi$-acceptors. The colored products were measured spectrophotometrically at 842 nm and 552 nm for TCNQ and CL, respectively. The different experimental conditions are optimized. The linearities for TCNQ and CL were $1.6{\;}\mu\textrm{g}/mL~32{\;}\mu\textrm{g}/mL$ and $6.4{\;}\mu\textrm{g}/mL~160{\;}\mu\textrm{g}/mL$, respectively and colors were produced in non-aqueous media. This report describes a simple and ra\pid method for the analysis of enoxacin.

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