• 제목/요약/키워드: 7-derivatives

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

  • 이기창;박수인;황용현;이광일;최봉종;정덕채
    • 한국응용과학기술학회지
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    • 제8권1호
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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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    • 제25권3호
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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.

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

  • 양만표;김기흥;나기정
    • 한국임상수의학회지
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    • 제15권2호
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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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    • 제27권4호
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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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    • 제13권4호
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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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유기 태양 전지 응용을 위한 새로운 카바졸계 고분자 합성 및 특성에 관한 연구 (Synthesis and Characterization of New Poly(2,7-Carbazole) Derivative for Organic Solar Cells)

  • 이상규;김희주;박송주;채은아;조정민;문상진
    • 한국신재생에너지학회:학술대회논문집
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    • 한국신재생에너지학회 2010년도 춘계학술대회 초록집
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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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    • 제17권2호
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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.

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

  • 고동수;이인원;임융호
    • Applied Biological Chemistry
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    • 제41권7호
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    • pp.550-555
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    • 1998
  • Fluoro-quinolone carboxilic acid 유도체에서, 탄소-불소간 one bond coupling constants는 위치와 무관하게 249 Hz에서 257 Hz 사이의 값을 갖는데, geminal 및 vicinal coupling constants는 위치에 따라 그 값의 차이가 많이 생긴다. 즉, seminal coupling constants는 6 Hz에서 23 Hz의 값을 보이고 vicinal coupling constants는 1.9 Hz에서 7 Hz의 값을 보인다. 또한 수소-불소간 three bond coupling constants는 9 Hz에서 10.3 Hz의 값을 보이고, four bond coupling constants는 6 Hz에서 8.3 Hz의 값을 보인다.

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4-(2-Chloroethyl) semicarbazide의 히드라존 유도체 합성:새로운 종류의 세포독성요법제 (Synthesis of Hydrazone Derivatives of 4-(2-Chloroethyl) semicarbazide : A New Class of Cytotoxic Agents)

  • El-Sabbagh, O.I.;El-Sadek, M.E.;Aboukull, M.E.;Shallal, H.M.
    • 대한화학회지
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    • 제53권1호
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    • pp.34-41
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    • 2009
  • 새로운 종류의 히드라존 유도체는 4-(2-chloroethyl) semicarbazides로 부터 합성되었고, 인간 두 뇌(U251)와 간(Hepg2)의 암세포 에 대해 항증식성을 보였다. 히드라존 화합물은 벤즈알데히드, 아세토 페논, 3-formylindole 유도체이다. 아세토페논 유도체중에 3e (p-methoxy substituted)와 and 3f (p-nitro substituted)는 Hepg2 세포 (각각I$C_{50}$ = 6 ,8 $\mu$g/mL) 에 대해 가장 높은 세포독성활성을 보인다. 3-Formylindole 유도체중에 4a (hydrazone of 3-formylindole)은 U251 (I$C_{50}$ = 21 $\mu$g/mL)와 Hepg2 (I$C_{50}$ = 7 $\mu$g/mL)에 강한 세포독성활성을 보인다.

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

  • Quan De;Shin Woonsup
    • 전기화학회지
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    • 제7권2호
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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.