4-肉桂酰阿魏酸苯酚酯衍生物的合成及其抗炎活性

Synthesis and Antiinflammatory Activity of Derivatives of 4 Cinnamoylferulic Acid Phenolic Ester

选择对环氧酶／５－脂氧酶和氧自由基具有抑制作用的苯乙烯酚作为先导物，设计合成了１２个４－肉桂酰阿魏酸苯酚酯目标物，其中８个化合物未见文献报道．经药理初筛结果表明，目标物（７ｇ）对角叉菜胶致大鼠足趾肿胀，二甲苯致小鼠耳廓肿胀和棉球致大鼠肉芽组织增殖有显著抑制作用．

On the basis of structural analysis,the styrenes with inhibitory activity of cyclooxygenase and 5 lipoxygenase as well as reactive oxygen species were selected as a lead compound.Twelve of the 4 cinnamoylferulic acid phenolic esters were designed and synthesized,eight of them were never reported in the literature.Preliminary pharmacological tests showed that the target compound (7g)possessed significant inhibitory effect on animal models such as the effects on swelling caused by xylene in mice (p.o.) ,paw edema induced by carrageenin in rats (p.o.) and formation of granuloma tissue induced by cotton pellet in rats (p.o.) respectively.