DESIGN, SYNTHESIS AND IN VITRO ANTIFUNGAL EVALUATION OF NOVEL TRIAZOLE DERIVATIVES

摘要

As a part of our continuing research on triazole derivatives antifungal agents, 10 novel target compounds containing 1,2,4-triazole moiety were synthesized and characterized by the spectroscopic analysis, and their in vitro antifungal activities against four phytopathogenic fungi were assayed systematically. Especially, compound 3c displayed excellent activity against F. graminearum with the median effective concentration value (EC50) of 5.03 mu g/mL, and the value was extremely close to that of tebuconazole (EC50 = 3.13 mu g/mL). Generally, for carbonyl compounds containing morpholine moiety, introducing 4-F to benzene ring obviously improved activities against most of tested fungi in varying degree.