新型杂环酰胺砜类化合物的合成、抑菌活性及构效关系研究

The emergence of increase heavy lost of bacterial diseases has posed a serious concern for pesticide professionals during the last decade, the application of most traditional pesticides has not proved very effective. As our ongoing search for novel sulfone compounds possessing antibacterial properties, on the basis of the acylamide fungcides lead compounds, design, synthesis, antibacterial activity, qualitative and quantitative SAR of novel sulfone derivatives containing heterocyclic(thiadiazole, oxadiazole) acylamide will be carried out. Spacial attention would be paid to bacterial leaf blight of rice, bacterial leaf streak of rice, tobacco bacterial wilt and bacterial wilt of solanaceae.Possible mechanism of high activity compound agains bacterial would be developed. Some high active, safe, easy to use, lower cost compounds are expected to be found. In a word, two lead compounds with high activity and one title compounds with potential field application would be developed.

本项目针对我国当前农经作物中细菌病害成灾重、部分药剂抗性严重和无特效防治药剂等现实问题，以现有酰胺类杀菌剂为先导，引入杂环活性基团进行先导设计和优化。开展新型酰胺杂环(噻二唑、噁二唑)砜类化合物的设计、合成与抑菌活性研究，对目标化合物进行定性和定量构效关系分析，进一步开展结构优化，筛选出对水稻细菌性条斑病、水稻细菌性条斑病、番茄青枯病和烟草青枯病等细菌病害活性更高、安全、易于使用、成本更低的化合物。预期发现2个农药新先导化合物，1个具有潜在应用前景的高活性化合物。

本项目针对我国当前农经作物中病害成灾重、部分药剂抗性严重和无特效防治药剂等现实问题，以现有杀菌剂为先导，引入杂环活性基团进行先导设计和优化。开展新型酰胺杂环(噻二唑、噁二唑)砜类化合物的设计、合成与抑菌活性研究，对目标化合物进行定性和定量构效关系分析，进一步开展结构优化，筛选出1个对水稻白叶枯病、番茄青枯病等病害具有较好活性的化合物，发表SCI 论文3篇。