摘要
目的:获得具备抗氧化、脱羧酶抑制作用及更好的药代动力学性质的新型丹参素类药物。方法:设计了2-甲基取代丹参素衍生物,并以藜芦醛为原料,通过3步反应获得了该目标化合物。所采用的方法避免了氰化物的使用,增加了反应的安全性,并采用抗凝血作用研究评价了所获得的2-甲基取代丹参素衍生物的防治心肌缺血作用。结果:合成反应三步总收率29.1%,所得到的化合物经评价具备抗凝血作用。结论:获得了一种具备一定抗凝血作用的新型活性丹参素衍生物,为其产业化研究与应用提供了依据。
To obtain a new type of drug from Danshensu with antioxidant and decarboxylase inhibition and better pharmacokinetic properties. Method: 2-methyl-substituted Danshensu derivatives was designed by us. Using veratraldehyde as raw materials, the target compounds are obtained by 3-step reaction. The method adopted avoids the use of cyanides and increases the safety of the reaction. The anticoagulant function of 2-methyl-substituted Danshensu derivatives were evaluated. Result: The total yield of the synthesized reaction was 29.1%, and the com-pound was evaluated with its anticoagulant effect. Conclusion: A new type of active Danshensu derivative was obtained, which had the function of anticoagulant.
作者
王黎
雷媛
张蕾
王丹
WANG Li;LEI Yuan;ZHANG Lei;WANG Dan(College of Pharmacy,Xi'an Medical University,Xi'an 710021,China)
出处
《化学工程师》
CAS
2019年第1期63-66,共4页
Chemical Engineer
基金
陕西省自然科学基础研究计划项目(2017JM8060)
西安医学院大学生创新创业训练计划项目(2018DC-62)
关键词
丹参素衍生物
Α-羟基酸
藜芦酮
抗凝血
Danshensu derivatives
α-hydroxy acid
veratone
anticoagulation