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新型防己诺林碱衍生物的合成、表征及抑菌活性。

Synthesis, characterization, and fungicidal activity of novel Fangchinoline derivatives.

机构信息

College of Science, Huazhong Agricultural University, Wuhan 430070, China.

College of Science, Huazhong Agricultural University, Wuhan 430070, China.

出版信息

Bioorg Med Chem. 2020 Dec 1;28(23):115778. doi: 10.1016/j.bmc.2020.115778. Epub 2020 Sep 23.

DOI:10.1016/j.bmc.2020.115778
PMID:33007609
Abstract

A series of new Fangchinoline derivatives with the carbamate moiety (compounds 1a-1l, 2a-2l) were synthesized by utilizing phenolic hydroxyl to react with isocyanate. The potential fungicidal activity of all the target compounds has been screened against six species of plant pathogen fungi, including Pp. adianticola (Phomopsis adianticola), A. adianticola (Altermaria adianticola), C. fructicola (Colletotrichum fructicola), P. theae (Pestalotiopsis theae), P. adianticola (Phoma adianticola), and G. zeae (Gibberella zeae). Almost all the derivatives showed better fungicidal activity than Fangchinoline. Compounds 1f, 1g, 1h, and 1k exhibited obviously better activity against G. zeae, and Pp. adianticola than Azoxystrobin. Especially compounds 1k displayed high fungicidal activity against G. zeae, Pp. adianticola, and P. theae.

摘要

一系列新的含氨基甲酸酯部分的防己诺林碱衍生物(化合物 1a-1l、2a-2l)通过利用酚羟基与异氰酸酯反应合成。所有目标化合物的潜在杀菌活性都已针对六种植物病原菌真菌进行了筛选,包括 Pp. adianticola(Phomopsis adianticola)、A. adianticola(Altermaria adianticola)、C. fructicola(Colletotrichum fructicola)、P. theae(Pestalotiopsis theae)、P. adianticola(Phoma adianticola)和 G. zeae(Gibberella zeae)。几乎所有的衍生物都表现出比防己诺林碱更好的杀菌活性。化合物 1f、1g、1h 和 1k 对 G. zeae 和 Pp. adianticola 的活性明显优于肟菌酯。特别是化合物 1k 对 G. zeae、Pp. adianticola 和 P. theae 表现出很高的杀菌活性。

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