Design, Synthesis, and Antifungal Evaluation of Novel Benzoxazole Derivatives Containing a 1,2,3-Triazole Moiety

2017 
For finding novel bioactive compounds with significant antifungal activities, 17 novel benzoxazole derivatives containing a 1,2,3-triazole moiety were synthesized by the copper(II) acetylacetonate-catalyzed cyclization reaction between 2-aminophenol derivatives and 1H-1,2,3-triazole-4-carbaldehyde derivatives (4a), which were prepared through three steps using aromatic amine as the starting material. Antifungal activities of the prepared compounds were evaluated against Botrytis cinerea (BC) and Fusarium Verticillium (FV). The test results indicated that compounds 5b, 5c, 5h, and 5n show good inhibitory effects on fungi. The preliminary structure–activity relationship is also discussed.
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