含酚酰腙类衍生物的合成及生物活性研究  

Synthesis and Biological Evaluation of AcylhydrazoneDerivatives Containing Phenol Moieties

作　　者：成玉洁 刘贞汝 谭志同 沈亚龙 王守信 盛筱[1] Cheng Yujie;Liu Zhenru;Tan Zhitong;Shen Yalong;Wang Shouxin;Sheng Xiao(School of Pharmaceutical Sciences,Jining Medical University,Rizhao 276826,China)

机构地区：[1]济宁医学院药学院,山东日照276826

出　　处：《云南化工》2023年第12期25-29,共5页Yunnan Chemical Technology

基　　金：山东省医药卫生科技发展计划项目(202113050717);济宁医学院大学生创新训练计划项目(cx2022115z)。

摘　　要：以羟基取代苯甲酸甲酯、水合肼以及羟基取代苯甲醛为原料,通过肼解、缩合两步反应得到16个含酚酰腙类化合物(D1-D16),其结构经核磁共振氢谱、碳谱确证,并测试了目标化合物对酪氨酸酶的作用以及抗氧化活性。初步测试结果表明,化合物D1、D8、D12与D15对酪氨酸酶有一定的抑制作用,而化合物D2和D6对酪氨酸酶有弱的激活效果;所有目标化合物均具有较好的清除ABTS自由基的活性,IC 50值均优于对照药物抗坏血酸;部分目标化合物具有优异的清除DPPH自由基的活性,明显强于对照药物抗坏血酸。Sixteen acylhydrazonederivatives containing phenol moieties(D1-D16)were obtained by using hydroxyl substituted methyl benzoates,hydrazine hydrate and hydroxy substituted benzaldehydes as raw materials through two step reaction of hydrazinolysis and condensation.Their structures were confirmed by 1H NMR and 13 C NMR.The effects of the target compounds on tyrosinase and their antioxidant activities were tested.The preliminary test results showed that compounds D1,D8,D12 and D15 had a certain inhibitory effect on tyrosinase,while compounds D2 and D6 had a weak activation effect on tyrosinase.All the target compounds showed good ABTS free radicals scavenging activity,and the IC 50 values were better than that of the positive controlascorbic acid.Some of the target compounds had excellent DPPH free radicals scavenging activity,which were significantly stronger than the positive controlascorbic acid.

关 键 词：酪氨酸酶 抗氧化 合成 酚 酰腙 

分 类 号：O625.3[理学—有机化学]