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Design, synthesis and structure-activity relationship of novel coumarin derivatives
Ai-Ying Guan1, Chang-Ling Liu, Miao Li
1State Key Laboratory of the Discovery and Development of Novel Pesticide, Shenyang Research Institute of Chemical Industry, Shenyang, China.
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.
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