Design, synthesis and structure-activity relationship of novel coumarin derivatives |
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| Authors: | Guan Ai-Ying Liu Chang-Ling Li Miao Zhang Hong Li Zhi-Nian Li Zheng-Ming |
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| Affiliation: | State Key Laboratory of the Discovery and Development of Novel Pesticide, Shenyang Research Institute of Chemical Industry, Shenyang, China. |
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| Abstract: | BACKGROUND: The lead coumarin derivative (E)‐methyl 3‐methoxy‐2‐[2‐(4‐methylcoumarin‐7‐yloxymethyl)phenyl]acrylate was discovered by using an intermediate derivatisation method. To discover new coumarin derivatives with improved activity, a series of substituted coumarins were synthesised and bioassayed. RESULTS: The compounds were identified by 1H NMR, IR, MS and elemental analysis. Bioassays demonstrated that some of the title compounds exhibited excellent fungicidal activity against cucumber downy mildew at 25 mg L?1. The relationship between structure and fungicidal activity is reported. CONCLUSION: The present work demonstrates that coumarin derivatives containing methoxyacrylate moieties can be used as possible lead compounds for developing novel fungicides. Copyright © 2011 Society of Chemical Industry |
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| Keywords: | coumarin derivatives methoxyacrylates intermediate derivatisation method fungicidal activities structure‐activity relationship |
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