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天然黄樟素作为黄樟油的主要成份是一种丰富的于然产物,本文描述了由此而得的新硫茚酸3类似物(Z)-5,6-亚甲双氧基-2-甲基-1-(对-甲基硫酸基苯亚甲基)-3-茚基乙酸1的化学合成.该合成路线的主要特点有:短捷,立体选择性好,总产率高.由天然产物制备新类似物的总产率约为30%,结果如下:化合物1及相应的硫醚化合物12具有抗炎活性;12是1的合成前体,很可能也是1的重要代谢产物.对这些行生物在由鹿角莱引发的鼠瓜水肿试验的抗炎活性剖析显示:在剂量为42mg/kg,1,23mg/kg 13时,有效率为 50%,证实了这类试大的构效关系.结果显示,新类似物 1可能是一种具有与药物3相似治疗性质的前药.
Natural safrole sassafras as the sassafras oil is a major component of natural products, this article describes the resulting neoinmusic acid 3 analog (Z) -5,6-methylene-2-oxy-methyl Synthesis of 1 - (p - methylsulfanylidene) -3 - indenylacetic acid 1. The main features of this synthetic route are: short run, good stereoselectivity and high total yield. The overall yield of novel analogs for product preparation was about 30% with the following results: Compound 1 and the corresponding thioether compound 12 have anti-inflammatory activity; and 12 is a synthetic precursor of 1, probably also an important metabolite of 1. For these Analysis of the anti-inflammatory activity of the line organism in the rat and rat edema triggered by the antler Leptospira showed that the effective rate was 50% at doses of 42 mg / kg, 1, 23 mg / kg 13, confirming the structure-activity relationship The results show that the new analog 1 may be a prodrug with similar therapeutic properties as the drug 3.