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瑞香狼毒中分离出的瑞香新醇类似物的先导优化及杀虫活性

Lead optimization and insecticidal activity of analogues of daphneolone isolated from Stellera chamaejasme L.

作者信息

Chen Lin, Wang Xinliang, Lu Tao, Hou Taiping

机构信息

Key Laboratory of Bio-Resource and Eco-environment, Ministry of Education, College of Life Sciences, Sichuan University, Chengdu 610064, China.

出版信息

Pest Manag Sci. 2007 Sep;63(9):928-34. doi: 10.1002/ps.1399.

DOI:10.1002/ps.1399
PMID:17575567
Abstract

Starting from the chemical structure of the botanical aphicides 1,5-diphenyl-1-pentanone and 1,5-diphenyl-2-penten-1-one, extracted from Stellera chamaejasme L., the authors designed and synthesized a series of novel compounds following the concept of bioisosterism. Their structures were established on the basis of (1)H NMR and GC-MS spectra, and the insecticidal activities of the compounds were evaluated against Aphis gossypii Glover. The results demonstrated that the substitution of a heterocycle for the phenyl ring was favourable. Thus, further modification of compound 2n, containing a furan ring, which showed excellent activity (LC(50) = 0.85 g L(-1)), is of some promise.

摘要

从瑞香狼毒中提取的植物源杀蚜剂1,5 - 二苯基 - 1 - 戊酮和1,5 - 二苯基 - 2 - 戊烯 - 1 - 酮的化学结构出发,作者依据生物电子等排体概念设计并合成了一系列新型化合物。通过¹H NMR和GC - MS光谱确定了它们的结构,并针对棉蚜对这些化合物的杀虫活性进行了评估。结果表明,用杂环取代苯环是有利的。因此,对含有呋喃环且表现出优异活性(LC₅₀ = 0.85 g L⁻¹)的化合物2n进行进一步修饰具有一定前景。

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