• 제목/요약/키워드: Substituted

검색결과 3,533건 처리시간 0.024초

Synthesis of 6'-Substituted Dobutamine Analogues

  • Yoon, Sung-Hwa
    • Archives of Pharmacal Research
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    • 제15권3호
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    • pp.191-195
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    • 1992
  • Two 6'-substituted dobutamine analogues (1, 2) were synthesized from the coupling reaction of dopamine with the corresponding ketones. The ketone (8) was obtained from 4-nitrosalicyladehyde via 6 synthetic steps while the ketone (12) was prepared from 2-methyl-5-nitrobenzoic acid via 7 synthetic steps. Another synthetic attempts were also reported.

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Synthesis and Biological Activity of Indazole-Derived HMG-CoA Reductase Inhibitors

  • Kim, Jin-Il;Jahng, Yurng-Dong
    • Archives of Pharmacal Research
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    • 제18권3호
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    • pp.206-212
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    • 1995
  • New hypolipaemic agents, in which substituted indazole nucleus is connected to tetrahydro-4-hydroxy-2H-pyran-2-one by a two-carbon bridge, were designed and synthesized to show significant inhibitory activity against microsomal HMG-CoA reductase in rat liver.

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Synthesis of Substituted Phenyltrichlorocyclopropene Derivatives Using Friedel-Crafts Reaction

  • Choi, Sam-Kwon;Suk ,Won-Kyung
    • Bulletin of the Korean Chemical Society
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    • 제2권3호
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    • pp.83-85
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    • 1981
  • Tetrachlorocyclopropene has been prepared smoothly by the dehydrochlorination of pentachlorocyclopropane which could be obtained easily from sodium trichloroacetate and trichloroethylene in 1,2-dimethoxyethane. By the reaction of aromatic hydrocarbons with tetrachlorocyclopropene and aluminium chloride, new substituted phenyltrichlorocyclopropene derivatives have been prepared. The structures of these compounds were characterized by means of spectroscopic methods.

Synthesis of N-Substituted Isoindolin-1-ones via Palladium-Catalyzed Carbonylative Heterocyclization of o-Bromobenzylbromide with Carbon Monoxide and Primary Amines

  • 심상철;Li Hong Jiang;이동엽;조찬식
    • Bulletin of the Korean Chemical Society
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    • 제16권11호
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    • pp.1064-1067
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    • 1995
  • A convenient method for the synthesis of N-substituted isoindolin-1-ones is disclosed in palladium(0)-catalyzed heterocyclization of o-bromobenzylbromide with carbon monoxide (CO) and primary amines in DMF at 100 ℃.

Potential Antitumor ${\alpha}$-methylene-${\gamma}$-butyrolactone-bearing nucleic acid bases. 2. synthesis of $5^I-Methyl-5^I$-[2-(5-substituted uracil-1-yl)ethyl]-$2^I-oxo-3^I$-methylenetetrahydrofurans

  • Kim, Jack-C.;Kim, Ji-A;Park, Jin-Il;Kim, Si-Hwan;Kim, Seon-Hee;Choi, Soon-Kyu;Park, Won-Woo
    • Archives of Pharmacal Research
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    • 제20권3호
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    • pp.253-258
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    • 1997
  • Ten, heretofore unreported, $ 5^I-methyl-5^I-[2-(5-substituted uracil-1-yl)ethyl)]-2^I-oxo-3^I$-methylenetetrahydrofurans (H, F, Cl, Br, I, $ CH_3$,$CF_3$,$CH_2CH_3$,$ CH=CH2$, SePh) (7a-j) were synthesized and evaluated against four cell lines (K-562, FM-3A, P-388 and U-937). For the preparation of ${\alpha}$-methylene-${\gamma}$-butyrolactone-linked to 5-substituted uracils (7a-j), the convenient Reformasky type reaction was employed which involves the treatment of ethyl ${\alpha}$-(bromomethyl)acrylate and zinc with the respective 1-(5-substituted uracil-1-yl)-3-butanone (6a-j). The 5-substituted uracil ketones (6a-j) were directly obtained by the respective Michael type reaction of vinyl methyl ketone with the $K_2CO_3$(or NaH)-treated 5-substituted uracils (5a-j) in the presence of acetic acid in the DMF solvent. The .alpha.-methylene-.gamma.-butyrolactone compounds showing the most significant antitumor activity are 7e, 7f, 7h and 7j (inhibitory concentration $(IC_50)$ ranging from 0.69 to $2.9 {\mu}g/ml$), while 7b, 7g and 7i have shown moderate to significant activity. The compounds 7a, 7c and 7d were found to be inactive. The synthetic intermediate compounds 6a-j were also screened and found marginal to moderate activity where compounds 6b and 6g showed significant activity $(IC_50:0.4~2.8 {\mu}g/ml)$.

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난소화성 전분의 대체수준을 달리한 호두 빵의 품질 특성 연구 (Quality Characteristics of the Walnut Bread with Varied Levels of Resistant Starch)

  • 강남이;김혜영;이인선
    • 한국식생활문화학회지
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    • 제21권3호
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    • pp.290-296
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    • 2006
  • 본 연구에서는 난소화성 전분의 대체비율을 0%, 10%, 20% 및 30%로 하여 호두 빵을 제조하고 이화학적 검사, 관능검사 및 기호도 검사를 통하여 품질 특성을 조사하였다. 반죽의 pH는 10% 시료군과 대조군이 높은 값을 나타내었다. 반죽의 수분함량은 난소화성 전분을 대체한 시료군이 대조군에 비해 유의적으로 높은 값을 나타내었다. 완성된 빵의 부피는 대조군이 가장 큰 것으로 평가되었으나 10%와 20% 시료군과는 유의적인 차이를 보이지 않았다. 빵의 밝은 정도는 난소화성 전분을 대체한 비율이 높을수록 유의적으로 낮게 평가되었다. 빵의 경도는 10%와 20% 시료군이 대조군보다 유의적으로 낮은 특성을 나타내었다. 빵의 검성과 깨짐성은 비슷한 경향을 보이며 대조군과 30% 시료군이 강하게 평가되었다. 빵의 관능검사를 실시한 결과 고소한 맛은 대조군이 가장 특성이 강하게 평가되었고 떫은맛은 난소화성 전분의 대체비율이 높아짐에 따라 유의적으로 증가하는 것으로 나타내었다. 난소화성 전분의 대체비율이 높아질수록 떫은맛이 강해지므로 향후 떫은맛을 개선시키는 연구가 필요하다고 사료된다. 빵의 질긴 정도는 10%와 20% 시료군이 대조군보다 유의적으로 낮은 특성을 나타내어 부드럽게 평가되었다. 빵 내부의 조밀성은 대조군이 높게 평가되었으나 30% 시료군과는 유의적인 차이를 보이지 않았다. 빵의 기호도 검사 결과 조직감의 기호도는 10% 시료군이 대조군보다 유의적으로 높은 기호도를 나타내었다. 난소화성 전분으로 10%와 20%로 대체된 빵은 대조구와 비교하였을 때 유의적인 차이가 없거나 유의적으로 높은 기호도를 나타내어 개발 가능성을 보여주었으며, 아울러 품질 향상을 위한 체계적인 후속 연구가 계속 이루어져야 할 것으로 사료된다.