海洋生物碱aaptamines及其衍生物的设计、合成及生物活性研究

项目名称： 海洋生物碱aaptamines及其衍生物的设计、合成及生物活性研究

项目编号： No.21302038

项目类型： 青年科学基金项目

立项/批准年度： 2014

项目学科： 数理科学和化学

项目作者： 卢爱党

作者单位： 河北工业大学

项目金额： 25万元

中文摘要： 本项目系统开展海洋生物碱aaptamines植物病原菌抑制剂的新课题研究。探索简洁实用的全合成路线来大量制备aaptamines及其衍生物，在此基础上进行结构改造与修饰。通过将各类化合物进行系统的抗植物病原菌活性测试，总结构效关系，开展结构再优化，以期发现先导化合物。深入研究高活性先导化合物抑制植物病原菌的作用机理，扩大防治对象，优选实用有效的防治方法。对优选的先导化合物进行一级毒性和Ames毒性试验以及田间小区试验，评估其应用前景。该项目立题密切结合我国缺乏高效、低毒植物病原菌抑制剂的实际，期望创制出具有我国自主知识产权的、易于合成、有开发价值的高活性抗植物病原菌农药新品种，具有非常重要的理论和实际意义。

中文关键词： 生物碱aaptamine；全合成；杀菌活性；抗烟草花叶病毒活性；构效关系

英文摘要： A systematic research on the design, synthesis, antifungal activity and structure-activity relationship of the marine alkaloids aaptamines was carried out in this project. In order to thoroughly study the structure-activity relationship of these alkaloids, we plan to explore novel and practical synthetic routes for the large-scale synthesis of aaptamines and their derivatives. Then we will systematically modify and optimize these alkaloids using the developed synthetic route and evaluate the structure-activity relationship to find good pharmacophore and lead compounds. And then we will study the antifungal mechanism of these alkaloids using the optimum compound to enlarge the scope of prevention and optimize practic protection measure. For the next, the lead compounds will be tested for their toxicity and field plot activity to evaluate their application value. This project closely combines with the actual condition that there is lack of high efficiency and low toxicity antifungal agents in China, and expects to create a new antifungal agent with high efficiency,easy synthesis and independent intellectual property right. Therefore the project is of great importance and necessity.

英文关键词： aaptamine；total synthesis；antifungal activity；antiviral activity；structure activity