摘要：白藜芦醇是一种具有多种生物活性的天然产物，例如:抗癌、抗凝血、抗氧化活性，是近年研究中的一个热点，白藜芦醇目前已被开发成为第三代保健产品。但因其存在着这些或那些的缺陷，如其羟基结构易被氧化，使其极不稳定，限制了它在药物方面的应用前景。而它的某些衍生物拥有着比其更好的活性，也更稳定，所以近几年来，人们更倾向于结构修饰的研究。68802

本论文以白藜芦醇作为起始原料，用含氮、含硫杂环化合物对其结构进行修饰，共合成了5种新型结构的白藜芦醇杂环衍生物（4a-4e）， 通过1H NMR、13C NMR、HR-MS对化合物结构进行表征，并对5种合成的化合物进行了抗凝血生物活性测试，其中化合物4c抑制率为80.15%，呈现出一定的生物活性，对其进行体外凝血酶IC50值测试。结果表明化合物4c抗凝血活性 (IC50=10.43μM)好于白藜芦（IC50=25.87μM），其对凝血酶的抑制效果是白藜芦醇的两倍多，有望作为潜在的候选化合物，开展进一步的研究和开发，有望成为治疗心脑血管疾病的候选研发药物。

毕业论文关键词：白藜芦醇；白藜芦醇衍生物；合成；生物活性；凝血活性

Synthesis and Bioactivity of Resveratrol Derivatives 

Abstract: Resveratrol is a natural product with a variety of biological activities, such as anticancer, anticoagulant, antioxidant activity, is a hot spot in recent years, resveratrol has been developed into a third generation of health care product. But because of the existence of these or those defects, such as its hydroxyl structure easily oxidized, making it extremely unstable, limiting its application in the pharmaceutical prospects. And some of its derivatives have a better activity than it is, and more stable, so in recent years, people are more inclined to structural modification of the study.

In this paper, resveratrol was used as the starting material, and its structure was modified with nitrogen and sulfur containing heterocyclic compounds. Five new resveratrol heterocyclic derivatives (4a-4e) were synthesized and synthesized. 1H NMR, 13C NMR and HR-MS were used to characterize the structures of the compounds. Five compounds were tested for their anticoagulant biological activity. The inhibition rate of compound 4c was 80.15%, showing a certain biological activity. In vitro thrombin IC50 value test. The results showed that the anticoagulant activity of compound 4c (IC50 = 10.43μM) was better than that of veratrum (IC50 = 25.87μM), and its inhibitory effect on thrombin was more than twice that of resveratrol and was expected as a potential candidate compound, To carry out further research and development, is expected to become the treatment of cardiovascular and cerebrovascular disease candidate drug research and development.

Key Words: Resveratrol、Resveratrol derivatives 、Synthesis、Biological activity、Coagulation activity

目 录

1 前言 1

1.1 研究背景 1

1.2 白藜芦醇的来源、结构以及理化性质 2

1.2.1白藜芦醇的结构及性质