Design Synthesis and Antifungal Activity of Coumarin Ring-Opening Derivatives

摘要

Based on our initial design, we synthesized two series of coumarin ring-opening derivatives by the reactions of hydrolysis and methylation. Results of antifungal screening in vitro showed that the target compounds exhibited potent activity against the six common pathogenic fungi. Compounds >6b, >6e, >6g, >6i, >7b and >7c were identified as the most active ones, and the EC50 values of these active compounds were further tested. Compared to the commonly used fungicide Azoxystrobin (0.0884 µM), compounds >6b (0.0544 µM) and >6e (0.0823 µM) displayed improved activity against Botrytis cinerea.