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Paper | Regular issue | Vol 100, No. 5, 2020, pp.781-789
Published online, 2nd April, 2020
DOI: 10.3987/COM-20-14247
Design, Synthesis and in vitro Antifungal Evaluation of Novel Triazole Derivatives

Guoqing Sui,* Li Ren, Ruiyuan Liu, Dan Xu, Hongdong Hao,* and Wenming Zhou*

*College of Chemistry & Pharmacy, Northwest A & F University, No. 22 Xinong Road, Yangling, Shaanxi Province 712100, China

Abstract

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 µg/mL, and the value was extremely close to that of tebuconazole (EC50 = 3.13 μg/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.