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首页> 外文期刊>Bioorganic and Medicinal Chemistry Letters >Synthesis and inhibitory activity against COX-2 catalyzed prostaglandin production of chrysin derivatives.
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Synthesis and inhibitory activity against COX-2 catalyzed prostaglandin production of chrysin derivatives.

机译：合成和抑制活性对COX-2催化前列腺素的菊花衍生物的生产。

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摘要

A series of chrysin derivatives were prepared and evaluated for their inhibitory activities of cyclooxygenase-2 catalyzed prostaglandin production. Chrysin derivatives were prepared from 2-hydroxyacetophenone, 2,4-dihydroxyacetophenone and 2,6-dihydroxyacetophenone in 2 to 4 steps, respectively. Methxoylated chrysin derivatives were converted to the corresponding hydroxylated chrysin derivatives by the reaction with BBr(3) in good yields. The inhibitory activity of the chrysin derivatives against prostaglandin production from lipopolysaccharide-treated RAW 264.7 cells was measured. We found that chrysin derivatives with 3',4'-dichloro substituents (5e, 6e and 7e) exhibited good inhibitory activity of prostaglandin production.
机译：制备了一系列的chrysin衍生物，并评估了其对环氧合酶-2催化的前列腺素生产的抑制活性。由2-羟基苯乙酮，2，4-二羟基苯乙酮和2，6-二羟基苯乙酮分别以2至4个步骤制备Chrysin衍生物。通过与BBr（3）的反应以高收率将甲乙氧基化的菊花衍生物转化为相应的羟基化的菊花衍生物。测量了Chrysin衍生物对由脂多糖处理的RAW 264.7细胞产生的前列腺素的抑制活性。我们发现具有3'，4'-二氯取代基（5e，6e和7e）的菊花衍生物对前列腺素的生产具有良好的抑制作用。

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