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首页> 外文期刊>Bioorganic and Medicinal Chemistry >6-Acyl-4-aryl/alkyl-5,7-dihydroxycoumarins as anti-inflammatory agents
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6-Acyl-4-aryl/alkyl-5,7-dihydroxycoumarins as anti-inflammatory agents

机译：6-酰基-4-芳基/烷基-5,7-二羟基香豆素作为抗炎药

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摘要

A series of coumarin derivatives were synthesized in two steps from phloroglucinol. The anti-inflammatory activities of these derivatives were evaluated by means of inhibiting NO production in LPS-induced RAW 264.7 cells. Derivatives 3, 8, 10, 11, and 13 exhibited low micromolar levels of anti-inflammatory activities, and these derivatives also protected DNA against hydroxyl radical attack. Coumarin derivative 8 was the most potent derivative among those tested herein against NO production in LPS-induced RAW 264.7 cells with an IC_(50) value of 7.6 μM, and it effectively reduced the hydroxyl radical production by 50% at 100 μM in the electron spin resonance study.
机译：从间苯三酚分两步合成了一系列香豆素衍生物。通过抑制LPS诱导的RAW 264.7细胞中NO的产生来评估这些衍生物的抗炎活性。衍生物3、8、10、11和13表现出较低的微摩尔水平的抗炎活性，这些衍生物还可以保护DNA免受羟基自由基的攻击。香豆素衍生物8是本文测试的那些对抗LPS诱导的RAW 264.7细胞中NO产生的最有效衍生物，IC_（50）值为7.6μM，并且在电子中100μM时，其羟基自由基产生有效降低了50％自旋共振研究。

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