College of Science, Huazhong Agricultural University, Wuhan 430070, China.
National Biopesticide Engineering Research Center, Hubei Biopesticide Engineering Research Center, Hubei Academy of Agricultural Science, Wuhan 430064, China.
Molecules. 2019 Apr 3;24(7):1304. doi: 10.3390/molecules24071304.
A series of novel 3-aryl-4-hydroxy-2(5) furanone-acrylate hybrids were designed and synthesized based on the natural butenolides and acrylates scaffolds. The structures of the prepared compounds were characterized by ¹H-NMR, C-NMR and electrospray ionization mass spectrometry (ESI-MS), and the bioactivity of the target compounds against twelve phytopathogenic fungi was investigated. The preliminary in vitro antifungal activity screening showed that most of the target compounds had moderate inhibition on various pathogenic fungi at the concentration of 100 mg·L, and presented broad-spectrum antifungal activities. Further studies also indicated that compounds and still showed some inhibitory activity against , and on rape plants at lower concentrations, which could be optimized as a secondary lead for further research.
基于天然丁烯内酯和丙烯酸盐骨架，设计并合成了一系列新型 3-芳基-4-羟基-2(5)呋喃酮-丙烯酸盐杂合化合物。通过 ¹H-NMR、C-NMR 和电喷雾电离质谱（ESI-MS）对所制备的化合物进行了结构表征，并对目标化合物对 12 种植物病原菌的生物活性进行了研究。初步的体外抗真菌活性筛选表明，大多数目标化合物在 100mg·L 的浓度下对各种病原菌真菌具有中等抑制作用，表现出广谱抗真菌活性。进一步的研究还表明，化合物 和 在较低浓度下对 、 和 仍表现出一定的抑制活性，可作为进一步研究的次级先导化合物进行优化。
