State Key Laboratory of the Discovery and Development of Novel Pesticide, Shenyang Research Institute of Chemical Industry, Shenyang, China.
Pest Manag Sci. 2011 Jun;67(6):647-55. doi: 10.1002/ps.2103. Epub 2011 Feb 9.
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.
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.
The present work demonstrates that coumarin derivatives containing methoxyacrylate moieties can be used as possible lead compounds for developing novel fungicides.
通过采用中间体衍生化方法，发现了先导香豆素衍生物（E）-甲基 3-甲氧基-2-[2-（4-甲基香豆素-7-基氧甲基）苯基]丙烯酸酯。为了发现具有更好活性的新型香豆素衍生物，合成了一系列取代的香豆素并进行了生物测定。
通过 ¹H NMR、IR、MS 和元素分析鉴定了化合物。生物测定表明，一些标题化合物在 25mgL⁻¹浓度下对黄瓜霜霉病表现出优异的杀菌活性。报道了结构与杀菌活性之间的关系。
本工作表明，含有甲氧基丙烯酸酯部分的香豆素衍生物可用作开发新型杀菌剂的潜在先导化合物。
