新型桃金娘烯醛基生物活性化合物的合成及构效关系研究

项目名称： 新型桃金娘烯醛基生物活性化合物的合成及构效关系研究

项目编号： No.31460173

项目类型： 地区科学基金项目

立项/批准年度： 2015

项目学科： 农业科学

项目作者： 段文贵

作者单位： 广西大学

项目金额： 50万元

中文摘要： 以α-蒎烯烯丙位甲基氧化得到的桃金娘烯醛为原料，将其进一步氧化为桃金娘烯酸，然后采用亚结构连接法，通过桃金娘烯酸羧基的改性反应，设计和合成桃金娘烯醛基噻二唑-酰胺化合物、桃金娘烯醛基噻二唑-硫脲化合物、桃金娘烯醛基双1,3,4-噁二唑化合物、桃金娘烯醛基酰胺-磺酰胺化合物和桃金娘烯醛基酰腙化合物等五类未见文献报道的桃金娘烯醛基生物活性化合物，实现活性成分的优化叠加。探索合成条件，表征产物结构，测试生物活性(如抗菌、除草、植物生长调节、杀虫、抗病毒、与DNA相互作用等)，研究取代基结构与生物活性的关系，以期寻求具有生物活性的新的先导物质，为创制新的医药或农药打下基础，为我国天然优势资源松节油的改性和高值化利用提供新的途径。

中文关键词： 桃金娘烯醛；α-蒎烯；生物活性化合物；合成；构效关系

英文摘要： Myrtenic acid was prepared by oxidation of myrtenal which was produced via oxidation of allyl methyl in α-pinene. Then, five types of novel myrtenal-based bioactive compounds, i.e. myrtenal-based thiadiazole-amides, myrtenal-based thiadiazole-thioureas, myrtenal-based bis 1,3,4-oxadiazoles, myrtenal-based amide-sulfamides, and myrtenal-based acylhydrazones, will be designed and synthesized by using the substructure connection method and chemical modification reactions of the carboxy group in myrtenic acid, for realizing optimization and superposition of the active constituents. The synthetic conditions will be investigated, the structures of the products will be characterized, the bioactive activities including antimicrobial, herbicidal, plant growth regulating, insecticidal, antiviral, and interaction with DNA activities will be tested, and the substituent group-bioactivity relationship will be studied. This research project aims at finding novel leading compounds with bioative activities, providing fundamental data for the preparation of new medicine or pesticide, and openning a new pathway for the modification and high-value utilization of turpentine which is a natural and preponderant resource of China.

英文关键词： myrtenal;α-pinene;bioactive compound;synthesis;structure-activity relationship