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具有1H-吡唑-5-氧基侧链的新型嗜球果伞素衍生物的设计、合成及生物活性

Design, synthesis and biological activity of new strobilurin derivatives with a 1H-pyrazol-5-oxy side chain.

作者信息

Li Miao, Liu Chang-Ling, Yang Ji-Chun, Li Lin, Li Zhi-Nian, Zhang Hong, Li Zheng-Ming

机构信息

Agrochemical Discovery Department, Shenyang Research Institute of Chemical Industry, Shenyang 110021, China.

出版信息

Nat Prod Commun. 2009 Sep;4(9):1215-20.

PMID:19831032
Abstract

A series of new strobilurin derivatives with a substituted pyrazole side chain (5 and 6) were designed and synthesized. The new derivatives were synthesized from substituted phenones as starting material via esterification, cyclization and condensation reactions. All compounds were identified by 1H NMR and IR spectral and elemental analyses. Preliminary biological evaluation showed that some of the compounds had good fungicidal activity against cucumber downy mildew (CDM) and wheat powdery mildew (WPM) at 6.25 and 1.56 mg L(-1), respectively. Some of the compounds showed insecticidal activity against armyworm (AW), green peach aphid (GPA) and culex mosquitoes at 600 mg L(-1).

摘要

设计并合成了一系列带有取代吡唑侧链的新型甲氧基丙烯酸酯类衍生物(5和6)。这些新衍生物以取代苯乙酮为起始原料,通过酯化、环化和缩合反应合成。所有化合物均通过1H NMR、IR光谱和元素分析进行鉴定。初步生物活性评价表明,部分化合物在6.25和1.56 mg L(-1)浓度下,分别对黄瓜霜霉病菌(CDM)和小麦白粉病菌(WPM)具有良好的杀菌活性。部分化合物在600 mg L(-1)浓度下对粘虫(AW)、桃蚜(GPA)和库蚊具有杀虫活性。

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