以天然活性手性二氢异香豆素为模板，采用仿生合成策略，设计并合成5类共计102个3-烃基-3,4-二氢异香豆素类化合物，其中包含13个手性化合物。以13种常见植物病原真菌为供试菌，采用菌丝生长速率法系统测评各化合物的抗菌活性及抗菌谱，定性阐明供试化合物的2D和3D抗菌构效关系，建立分子结构参数与其抗菌EC50之间的数学模型。对活性好的化合物，通过安全性试验，从中筛选出对植物生长安全性高且抗菌活性强的目标化合物。对优选出的化合物，通过盆栽试验，评价其对敏感病原菌感染的防治效果及此类化合物作为新型植物抗菌药物的开发前景。该研究首次采用仿生合成策略展开对新型二氢异香豆素类化合物抗菌活性及其构效关系的系统性探索研究，其研究成果不仅将使人们首次认识一系列新型二氢异香豆素的抗菌活性及其构效关系，而且将为此类化合物的后续结构优化及未来创制新型二氢异香豆素类农用抗菌药物奠定理论基础并提供技术与方法参考。

One hundered and two 3-alkyl-3,4-dihydroisocoumarins containing 13 chiral ones will be designed and synthesized by employing a naturally active compound as the model molecule. Their antifungal activities and spectra against 13 types of phytopathogenic fungi will be evaluated using mycelium linear growth rate method. By association analysis of the structures of various compounds and their EC50 values, the qualitative and quantitative structure-activity relationships will be established. For the compounds with the higher activities, we will search for the ideal target compounds by safety testing, which should show fairly higher antifungal activities and are safe for the plant growth. For the ideal compounds, their control efficiency against the diseases caused by sensitive pathogenic fungi and the safety for plant growth will be explored through pot culture experiment. This study will be the first systematical investigation on the antifungal activity and structure-activity relationship of new chiral dihydroisocoumarins. The results will not only make people firstly understand the bioactivity and structure-activity relationship of a series of new dihydroisocoumarins, but also provide a theoretical base and methodological reference for their further structural optimization and the future development of new antifungal agent with dihydroisocoumarin skeleton.