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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Synthesis and anti-inflammatory evaluation of novel angularly or linearly fused coumarins.
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Synthesis and anti-inflammatory evaluation of novel angularly or linearly fused coumarins.

机译：新型角向或线性融合香豆素的合成和抗炎评估。

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摘要

Angular [7,8]-fused coumarins were obtained from the reaction of [2,3]-fused phenols with DMAD and PPh(3), while linear [6,7]-fused coumarins were formed from the analogous reaction of [3,4]-fused phenols with DMAD and PPh(3). These compounds were tested in vitro for antioxidant activity and they found to present significant scavenging activity. In parallel, these new compounds were evaluated in vivo for anti-inflammatory activity and they found to inhibit the carrageenin-induced paw edema (34-65%). Although their interaction with the free stable radical DPPH was low, the methyl 2,2-dimethyl-8-oxo-3,8-dihydro-2H-furo[2,3-h]chromene-6-carboxylate was the most potent (65%) in the in vivo experiment. The later seems to be a potent soybean Lipoxygenase inhibitor and does not acquire gastrointestinal toxicity.
机译：从[2,3]融合的苯酚与DMAD和PPh（3）的反应中获得角状[7,8]融合的香豆素，而由[3]的类似反应形成线性的[6,7]融合的香豆素。 ，4]-稠合的酚与DMAD和PPh（3）。在体外测试了这些化合物的抗氧化活性，发现它们具有明显的清除活性。同时，在体内评估了这些新化合物的抗炎活性，发现它们抑制了角叉菜胶诱导的爪水肿（34-65％）。尽管它们与自由基稳定自由基DPPH的相互作用较低，但是2,2-二甲基-8-氧代-3,8-二氢-2H-呋喃[2,3-h]色烯-6-羧酸甲酯是最有效的（ 65％）在体内实验中。后者似乎是一种有效的大豆脂氧合酶抑制剂，不会产生胃肠道毒性。

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