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目的合成多羟基口山酮及其脂肪胺基烷基衍生物,研究其抗氧化活性和构效关系。方法以邻甲氧基苯甲酸衍生物为起始原料,经酰氯化、Friedel-Crafts酰化、环合、脱甲基化及脂肪胺基烷基取代等反应合成目标化合物。以体外抑制Cu2+诱导的低密度脂蛋白(LDL)氧化和清除二苯代苦味肼自由基(DPPH)的EC50值检测目标化合物的抗氧化活性。结果共得到11个化合物(其中3个脂肪胺基烷基衍生物为新化合物),经IR、1H-NMR等确证其结构。初步药理试验结果表明,含邻二羟基的多羟基口山酮具有良好的抗氧化活性。结论邻二羟基的存在与口山酮衍生物的抗氧化活性有密切关系;羟基的取代数量对活性没有明显影响;取代位置对活性的影响有待进一步研究。
OBJECTIVE: To synthesize polyhydroxyl sophorone and its derivatives of fatty aminoalkyl, and study its antioxidant activity and structure-activity relationship. Methods The target compounds were synthesized by the reaction of o-methoxybenzoic acid derivatives with acyl chloride, Friedel-Crafts acylation, cyclization, demethylation and aliphatic aminoalkyl substitution. The anti-oxidative activity of the target compounds was tested in vitro by inhibiting the Cu2 + -induced LDL oxidation and clearing the EC50 value of dibenzyl bitter hydrazine free radicals (DPPH). As a result, a total of 11 compounds were obtained, of which 3 were aliphatic amidoalkyl derivatives and their structures were confirmed by IR, 1H-NMR and so on. Preliminary pharmacological test results show that o-dihydroxyl-containing hydroxyl ketone has good antioxidant activity. Conclusion The presence of ortho-dihydroxy is closely related to the antioxidant activity of the derivatives of the flavone. The number of substituted hydroxyl groups has no significant effect on the activity. The effect of substitution position on the activity remains to be further studied.