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Synthesis and biological evaluation of nonaprenylsulfates

机译:壬烯基硫酸盐的合成及生物学评价

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A naturally occurring nonaprenylsulfate (1) and its synthetic analogue (2) were synthesized from substituted phenolic precursors in three steps with an overall yield of 40-45%. Both compounds exhibited potent anti-inflammatory activity against 5-lipoxygenase, and potent brine shrimp lethality. They also showed moderate anti-oxidant activity in the super oxide radical scavenging model. Nonaprenylsulfate (1) showed moderate inhibition of paw edema in Freund's Complete Adjuvant (FCA) induced model of arthritis, thus confirming its anti-inflammatory activity.
机译:由取代的酚类前体分三步合成了天然存在的壬烯基硫酸盐(1)及其合成类似物(2),总产率为40-45%。两种化合物均显示出对5-脂氧合酶的有效抗炎活性,以及​​对虾盐水的致死性。他们还在超氧化物自由基清除模型中显示出适度的抗氧化活性。壬烯基硫酸盐(1)在弗氏完全佐剂(FCA)诱导的关节炎模型中显示了对足爪水肿的中等抑制作用,从而证实了其抗炎活性。

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