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Design, synthesis and structure–activity relationship of novel coumarin derivatives
Author(s) -
Guan AiYing,
Liu ChangLing,
Li Miao,
Zhang Hong,
Li ZhiNian,
Li ZhengMing
Publication year - 2011
Publication title -
pest management science
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.296
H-Index - 125
eISSN - 1526-4998
pISSN - 1526-498X
DOI - 10.1002/ps.2103
Subject(s) - coumarin , fungicide , chemistry , downy mildew , bioassay , lead compound , derivative (finance) , chemical structure , organic chemistry , stereochemistry , combinatorial chemistry , biology , in vitro , biochemistry , botany , economics , financial economics , genetics
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 1 H 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