Synthesis and Bio-Evaluation of Natural Butenolides-Acrylate Conjugates

A series of novel 3-aryl-4-hydroxy-2(5H) furanone-acrylate hybrids were designed and synthesized based on the natural butenolides and acrylates scaffolds. The structures of the prepared compounds were characterized by1H-NMR,13C-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−1, and presented broad-spectrum antifungal activities. Further studies also indicated that compounds7eand7kstill showed some inhibitory activity againstPestallozzia theae,Sclerotinia sclerotiorumandGibberella zeaeon rape plants at lower concentrations, which could be optimized as a secondary lead for further research.Keywords:3-aryl-4-hydroxy-2(5H)-furanone;butenolides;acrylate;antifungal activity;natural product