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新型(E)-α-(甲氧基亚氨基)苯乙酸酯衍生物的合成及生物活性,其中含有取代的吡唑环。

Synthesis and biological activity of new (E)-alpha-(Methoxyimino)benzeneacetate derivatives containing a substituted pyrazole ring.

机构信息

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

出版信息

J Agric Food Chem. 2010 Mar 10;58(5):2664-7. doi: 10.1021/jf9026348.

Abstract

Strobilurins are one of the most important classes of agricultural fungicides. To discover new strobilurin analogues with high activity, a series of new strobilurin derivatives containing a substituted pyrazole in the side chain were synthesized and their biological activities were tested. The compounds were identified by (1)H nuclear magnetic resonance, infrared, and elemental analysis. The test results indicated that the compounds exhibited strong fungicidal activities against Pyricularia oryzae , Phytophthora infestans , Pseudoperonospora cubensis , and Erysiphe graminis . The relationship between structure and biological activity is discussed in terms of the effects of the substituents on the pyrazole ring. The present work demonstrates that strobilurin analogues with a 3-(substituted phenyl)-1H-pyrazol-5-oxy side chain can be used as possible lead compounds for the development of potential agrochemicals.

摘要

烯肟菌酯是最重要的农用杀菌剂之一。为了发现具有高活性的新型烯肟菌酯类似物,我们合成了一系列含有取代吡唑侧链的新型烯肟菌酯衍生物,并测试了它们的生物活性。这些化合物通过 (1)H 核磁共振、红外光谱和元素分析进行了鉴定。测试结果表明,这些化合物对稻瘟病菌、马铃薯晚疫病菌、古巴假霜霉菌和禾谷白粉菌具有很强的杀菌活性。根据吡唑环上取代基的影响,讨论了结构与生物活性之间的关系。本工作表明,具有 3-(取代苯基)-1H-吡唑-5-氧基侧链的烯肟菌酯类似物可用作开发潜在农用化学品的可能先导化合物。

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