Design, synthesis and structure-activity relationship of novel coumarin derivatives
2011
Guan, Ai-Ying | Liu, Chang-Ling | Li, Miao | Zhang, Hong | Li, Zhi-Nian | Li, Zheng-Ming
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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