新型磺酰脲分子多功能生物活性的基础研究

Sulfonylurea herbicides are environmental benign herbicides which have been one of the hot research topics in recent decades because they have exhibited extremely low mammalian toxicity and ultra-high efficacy, ultra-low application rates and low environmental impact. Sulfonylurea herbicides containing mono-substituted pyrimidine moiety are orgianted from our invention and have been verified for years of field practices to retain the favourable characteristics as mentioned above. To advance our research interests, more novel sulfonylurea structures have recently been synthesized in our group among which some showed not only good herbicidal activity, but surprising impressing fungicidal activity. Meanwhile, the study on the residue regulation of sulfonylurea herbicides has significant importance to discover new sulfonyl urea herbicide to meet the special crop cultivation pattern (multiple crops on the same piece of land annually) existing in China . Accordingly the project will also cover the basic study on the molecular design, synthesis and multifunctional biological activity (herbicide, degradation, fungicide,sterilizer) of new sulfonylureas; establish or optimize the specific methods of sulfonylure degradation duration and multifunctional biological activitiesy; summarize the structure-activity relationship of new sulfonoylurea structures. This project will lay a broader insight in the sulfonylurea structures /biological in some new frontiers.

磺酰脲类除草剂具有超高效，用量极少，对温血动物几乎无毒，对环境友好的优点，具有绿色农药的特色，在近二十年来一直是研究的热点之一。含单取代嘧啶环的磺酰脲类是我们的发明专利，已从实践中验证其超高效的除草活性。近期我们合成的新磺酰脲类化合物生测表明除具有较好的除草活性外，也具有优异的抗菌活性，可作为先导化合物开展深入研究。同时，磺酰脲类除草剂的残留期调控研究对于开发符合我国国情的除草剂研究具有重要意义。据此，本课题将深入开展新磺酰脲类化合物的分子设计、合成以及除草、降解、抗菌的多功能生物活性研究；建立或完善模拟残留期及多功能生物活性测定方法；总结构效关系规律。本课题的开展将为磺酰脲类化合物的在多领域广泛深入研究奠定基础。

本项目开展基于AHAS靶标的磺酰脲类结构的合理分子设计工作，合成了多个系列计约400多个新化合物，主要测试了除草和抑菌等生物活性，发现了个别活性优异的化合物作为除草剂先导结构继续优化设计，磺酰基2, 6-位双取代的磺酰脲衍生物和芳基取代嘧啶基磺酰脲衍生物等; 同时发现具有抑菌多功能活性的磺酰脲类结构，如Aryl-5-烯基磺酰脲类结构；在磺酰脲类结构降解方面也取得了初步的探索结果。