• Title/Summary/Keyword: 7-derivatives

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Cinnamic Acid Derivatives IV, The Kinetics and Mechanism of the Hydrolysis of Cinnamylidene aniline Derivatives (신남산 유도체 Ⅳ, Cinnamylidene anilin 유도체의 가수분해 반응에 대한 메카니즘과 그 반응속도론적 연구)

  • Lee, Gi-Chang;Park, Su-In;Hwang, Yong-Hyeon;Lee, Gwang-Il;Choe, Bong-Jong;Jeong, Deok-Chae
    • Journal of the Korean Applied Science and Technology
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    • v.8 no.1
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    • pp.1-7
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    • 1991
  • The kinetic of hydrolysis for cinnamylidene aniline derivatives has been investigated by ultraviolet spectrophotometry in 20% (v/v) dioxane - $H_2O$ at $25^{\circ}C$. A rate equation which can be applied over wide pH range was obtained. The substituent effects on cinnamylidene aniline derivatives were studied and the hydrolysis was facilitated by electron attracting group. Final products of the hydrolysis were cinnamaldehyde and aniline. From the rate equation, substituent effect and final products, the hydrolysis of cinnamylidene aniline derivatives was initiated by the neutral molecule of $H_2O$ which does not dissociate at below pH 9.0${\sim}$12.0, but proceeded by the hydrogen ion at above pH 5.0${\sim}$9.0.

Synthesis of New 2-Thiouracil-5-Sulfonamide Derivatives with Biological Activity

  • Fathalla, O.A.;Zaghary, W.A.;Radwan, H.H.;Awad, S.M.;Mohamed, M.S.
    • Archives of Pharmacal Research
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    • v.25 no.3
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    • pp.258-269
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    • 2002
  • 2-Thiouracil-5-sulfonylchloride 1 reacted with a series of aromatic and heterocyclic amines to give 2a-j. The same compound 1 was reacted with a series of sulphonamides giving different sulphonamides of type 3a-e. On the other hand compound 1 was allowed to react with p-aminoacetophenone givining compound 4 which in turn was allowed to react with derivatives of alkyl thiosemicarbazides to give thiosemicarbazones of type 5a-e, also compound 4 was monobrominated to give compound 6 which in turn was reacted thiosemicarbazones of some aldehydes to give the corresponding thiazole derivatives 7a-f. In the same time compound 4 was reacted with a series of aromatic and heterocyclic aldehydes givining chalcones 8a-g (Claisen-Schemidt reaction). Also compound 4 was allowed to react with a series of aromatic and heterocyclic aldehydes, ethyl cyano acetate and/or malononitrile, and ammonium acetate giving pyridine derivatives 9a-d and 10a-e respectively. The biological effects of some of the new synthesized compounds was also investigated.

Effects of Chicken Egg White Derivatives on Neutrophil Phagocytosis in the Rats (랫드의 호중구 탐식능에 있어서 계난백유래물질의 효과)

  • 양만표;김기흥;나기정
    • Journal of Veterinary Clinics
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    • v.15 no.2
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    • pp.352-357
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    • 1998
  • Effects of chicken egg white derivatives (EWD and EF-203) on the changes of blood cells and the neutrophil phagocytic activity were examined in the rats. Rats were administered orally with either EWD (200 mg/kg) or EF-203 (200 mg/kg) for 3 days. Thereafter, the changes of blood cell values (RBC, WBC, platelets, PCV, differential count of neutrophils) and the phagocytic activity of neutrophils were evaluated for 7 days. The numbers of WBC and the differential count of neutrophils of rats administered with either EWD or EF-203 were significantly increased (p

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Xanthone and Flavonoid Derivatives from the Leaves of Maclura tricuspidata with Antioxidant and Anti-tyrosinase Activity

  • Jo, Yang Hee;Lee, Solip;Ryu, Se Hwan;Yeon, Sang Won;Turk, Ayman;Hwang, Bang Yeon;Lee, Mi Kyeong
    • Natural Product Sciences
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    • v.27 no.4
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    • pp.234-239
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    • 2021
  • Masclura tricuspidata, also called as Cudrania tricuspidata, is one of the most common Moraceae family plants in East Asia. Its trivial name follows mulberry due to the similar morphology. Investigation of the bioactive constituents of M. tricuspidata leaves yielded a new xanthone derivative along with twenty known compounds through various chromatographic techniques. A new compound was defined as mascluraxanthone (3), a prenylated xanthone glucoside on the basis of 1D and 2D NMR and MS data. Twenty known compounds were identified as four xanthone derivatives (1-2 and 4-5), two flavans (6-7), six flavanol derivatives (8-13), a flavonone (14) and seven flavonol derivatives (15-21). Among the isolated compounds, flavanol and flavonoid derivatives with 3',4'-OH groups showed antioxidant and anti-tyrosinase activities. Conclusively, the leaves of M. tricuspidata are rich in aromatic compounds including xanthones and flavonoids. In addition, these constituents showed antioxidant and anti-tyrosinase potentials, which might be useful for oxidative stress related diseases.

Bezoin in Heterocyle Synthesis: Synthesis and Reactions of 2, 3-Diphenyl-4-cyanopyrrole-5-thione

  • Khalifa, Fathy A.;Zohdi, Hussein F.;Ibrahim, M.K.A.;Ismail, N.A.
    • Archives of Pharmacal Research
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    • v.13 no.4
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    • pp.351-354
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    • 1990
  • 2, 3-diphenyl-4-cyano-pyrrole-5-thione (4) was either by the reaction of benzoin (1) and cyanothioacetamide (3) followed by cyclization using AcOH/sodium acetate or by refluxing a mixture of benzoin (1) and cyanothioacethamide in pyridine to afford directly 4. Several new pyrrole and pyrazole derivatives were synthesised using 4 as synthon. The structure of the newly synthesised derivatives were based on celemental and spectral data studies. Methylation of the SH group in 4 afforded 5. Reaction of 4 with ethyl bromo acetate afforded (6). Treatment of (5) and (6) with hydrazine hydrate afforded the same pyrazole derivative (10) through the intermediate (9). Treatment of 6 with aniline and phenylhydrazine afforded the pyrrole derivatives 8a, b respectively. Treatment of 6 while dill HCI gave 2, 3-diphenyl-4-cyano-pyrrole-5-one (7). Treatment of 6 with $NH_3$/EtOH afforded the amidic derivatives (11) with treatment of 6 $NH_3$/ heat then acidification it gave the carboxylic derivatives (12).

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Synthesis and Characterization of New Poly(2,7-Carbazole) Derivative for Organic Solar Cells (유기 태양 전지 응용을 위한 새로운 카바졸계 고분자 합성 및 특성에 관한 연구)

  • Lee, Sang Kyu;Kim, Hee Joo;Park, Song Joo;Chae, Eun Ah;Cho, Jung Min;Moon, Sang-Jin
    • 한국신재생에너지학회:학술대회논문집
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    • 2010.06a
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    • pp.73.2-73.2
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    • 2010
  • Polymer solar cells (PSCs) have attracted considerable academic and commercial interest because of their unique advantages, such as the facile manufacture of low cost, flexibility, lightweight, and solution processibility. Recently, high-performance polymer solar cells made from a mixture of poly(2,7-carbazole) derivatives, PCDTBT, and [6,6]-phenyl C71 butyric acid methyl ester (PC70BM) have been reported, with maximum power conversion efficiency of 6.1%. In this work, we report new novel copolymers based on poly(2,7-carbazole) derivatives with a suite of electron-deficient moieties or electron-rich units. We systematically investigated the synthesis, thermal stability, as well as the optical and electrochemical properties of these polymers. Detailed synthetic scheme, optical, electrochemical, and photovoltaic properties of the copolymers will be presented.

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Cytotoxicity of Ergosterol Derivatives from the Fruiting Bodies of Hygrophorus russula

  • Lee, Ik-Soo;Kim, Jin-Pyo;Na, Min-Kyun;Jung, Hyun-Ju;Min, Byung-Sun;Bae, Ki-Hwan
    • Natural Product Sciences
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    • v.17 no.2
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    • pp.85-89
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    • 2011
  • Bioassay-guided fractionation of the $CHCl_3$-soluble fraction of a MeOH extract of the fruiting bodies of Hygrophorus russula led to the isolation of five ergosterol derivatives (1 - 5). The structures of these compounds were identified as ergosterol peroxide (1), ergosta-4,6,8(14),22-tetraen-3-one (2), ergosta-7,22-diene-3${\beta}$,5${\alpha}$,6${\alpha}$-triol (3), ergosta-7,22-diene-3${\beta}$,5${\alpha}$,6${\beta}$,9${\alpha}$-tetraol (4), and 5${\alpha}$,6${\alpha}$-epoxy-ergosta-8(14),22-diene-3${\beta}$,7${\alpha}$-diol (5) by comparing their physicochemical and spectral data with those in the literature. These compounds were evaluated for in vitro cytotoxicity against A549 and XF498 cancer cell lines. Most of the tested compounds, except for compound 3, exhibited moderate cytotoxicity against both A549 and XF498 cell lines with $IC_{50}$ values ranging from 10.2 to 18.3 ${\mu}g/ml$ and from 11.4 to 24.6 ${\mu}g/ml$, respectively.

Survey of Carbon- and Proton-Fluorine Coupling Constants in Fluoro-quinolone Carboxylic Acid Derivatives (Fluoro-quinolone Carboxylic Acid 유도체로부터 탄소-불소 및 수소-불소간 Coupling Consstants의 조사)

  • Koh, Dong-Soo;Lee, In-Won;Lim, Yoong-Ho
    • Applied Biological Chemistry
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    • v.41 no.7
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    • pp.550-555
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    • 1998
  • For fluoro-quinolone carboxylic acid derivatives, one bond carbon-fluorine coupling constants are ranged from 249 Hz to 257 Hz regardless of positions. But geminal and vicinal carbon-fluorine coupling constants vary according to positions, namely, geminal coupling constants are ranged from 6 Hz to 23 Hz, and vicinal coupling constants are ranged from 1.9 Hz to 7 Hz. In cases of proton-fluorine couplings, three bond coupling constants are ranged from 9 Hz to 10.3 Hz, and four bond coupling constants ate ranged from 6 Hz to 8.3 Hz.

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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).

Amperometric Detection of Some Catechol Derivatives and o-aminophenol Derivative with Laccase Immobilized Electrode: Effect of Substrate Structure

  • Quan De;Shin Woonsup
    • Journal of the Korean Electrochemical Society
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    • v.7 no.2
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    • pp.83-88
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    • 2004
  • [ $DeniLite^{TM}$ ] laccase immobilized Pt electrode was used for amperometric detection of some catechol derivatives and o-aminophenol (OAP) derivative by means of substrate recycling. In case of catechol derivatives, the obtained sensitivities are 85, 79 and $57 nA/{\mu}M$ with linear ranges of $0.6\~30,\;0.6\~30\;and\; 1\~25 {\mu}M$ and detection limits (S/N=3) of 0.2, 0.2 and $0.3{\mu}M$ for 3,4-dihydroxycinnaminic acid (3,4-DHCA), 3,4-dihydroxybenzoic acid (3,4-DHBA) and 3,4-dihydroxyphenylacetic acid (3,4-DHPAA), respectively. In case of OAP derivative, the obtained sensitivity is $237 nA/{\mu}M$ with linear range of $0.2\~15{\mu}M$ and detection limit of 70 nM for 2-amino-4-chlorophenol (2-A-4-CP). The response time $(t_{90\%})$ is about 2 seconds for each substrate and the long-term stability is around 40-50days for catechol derivatives and 30 days for 2-A-4-CP with retaining $80\%$ of initial activity. The optimal pHs of the sensor for these substrates are in the range of 4.5-5.0, which indicates that stability of the enzymatically oxidized product plays a very important role in substrate recycling. The different sensitivity of the sensor for each substrate can be explained by the electronic effect of the sugstituent on the enzymatically oxidized form.