反抗性新烟碱杀虫剂的开发
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摘 要：作用于烟碱型乙酰胆碱受体（nAChRs）的新烟碱类杀虫剂自问世以来由于其活性高，杀虫谱广，对哺乳动物和水生动物毒性低，且有良好的内吸性及适当的田间稳定性而成为农药创制的重要热点领域。随着新烟碱类杀虫剂品种的大量频繁使用，已经产生了严重抗性，2005年稻飞虱对吡虫啉的抗性高达400倍以上，此外，由于频繁持续的使用，也对环境产生一定的负面影响，如，在欧洲和日本都相继发现吡虫啉对蜜蜂种群的影响，最高减少40%的蜜蜂数量，严重影响了作物花粉的传播。因此，从新的作用模型出发，针对业已出现的抗性问题和蜜蜂毒性，以提高生物选择性为切入点，开展靶向性的分子设计与合成，这对我国具有自主知识产权的新农药创制和农业害虫防治都具有重要意义。主要研究内容：（1）系统研究稻飞虱、烟粉虱等重大农业害虫对吡虫啉等新烟碱杀虫剂的抗性机制和基于分子靶标的作用模型；（2）以超高活性的顺硝烯化合物为基础，研究高活性的先导化合物生物合理性分子设计、先导结构多样性衍生与优化，创制顺硝烯反抗性新烟碱杀虫剂；（3）研究基于抗性机制的分子生物学和分子毒理学，建立与完善基于分子靶标的反抗性杀虫剂创制体系。预期目标：通过超高活性的先导化合物生物合理性分子设计、先导结构多样性衍生与优化研究，强化我国在顺硝烯反抗性新烟碱杀虫剂创制领域的优势。在活性化合物的基础上，开展基于抗性机制的分子生物学和分子毒理学研究，建立与完善基于分子靶标的反抗性机制杀虫剂创制体系。申请国际PCT专利，并进入指定国，进行高活性化合物的中试工艺研究，完成扩大杀虫谱试验和小区试验测试高活性化合物的急性经皮、经口、急性吸入、Ames试验、蜜蜂毒性等数据，为申请农药登记证做好前期工作。
关键词：反抗性 新烟碱 顺式构型
Abstract：Neonicotinoids acting on nAChRs have become the important hot-point research area because of its high bioactivities， broad spectrum， low toxicity to mammal and aquatic organisms， good systemic and suitable stability since they came into the market. With the using of large amount of neonicotinoids， the resistance is becoming very serious. The resistance ratio to imidacloprid aganist brown planthopper reached to 400 folds in 2005. In addition， frequent and continuous use result in negitive effect to the environment， for example， it was found in succession that imidacloprid influented the bee populations in Europe and Japan， the amount of bee decrease 40%， which affected seriously the spead of crop plllen. Therefore， based no the new model of action， targeting on the emerging resistance and bee toxicity， to improve the biological selectivity as the breakthrough point， we begin to target-orientation molecular design and synthesis， which is significant for the research and development of new pesiticde with independent intellectual property rights and the agricultural pest control. Main research content：（1）systemic research the resisitance mechanism and the model of action based on the molecular target of imidacloprid to planthopper and besimia tabaci etc. important agricultural pests；（2）Study the biological rational design of leading compounds with high activities， derivative and modification of lead structures based on the super high bioactivity of cis-configuration nitro methelene compounds and develop cis-configuration anti-resictance insecticide；（3）Study the molecular biology and toxicology based on the resistance mechanism and build and improve the research and development system of anti-resistance insecticides. Target： Through the study on the biological rational design of leading compounds with super high activities， derivative and modification of lead structures， the advantage of cis-configuration nitro methelene anti-resictance insecticide in our country is strengthened further. Based on the strucuture of the compound with activities， the researches on the molecular biology and toxicology based on the resistance mechanism are carried out and build and improve the research and development system of anti-resistance insecticides. To apply the PCT patent and come into the foreign countries， study the pilot process of the compound with hign activities， finish the experiments on broad spectrum and field trial， detemination the data of acute Acute percutaneous， acute through the mouth， acute inhalation， Ames test， bee toxicity， prepare the early stage work for the application of pesticide registration certificate.
Key Words：Anti-resistance；Neonicotinoids；Cis-configuration
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