Key Laboratory at Universities of Xinjiang Uygur Autonomous Region for Oasis Agricultural Pest Management and Plant Protection Resource Utilization, College of Agricultural, Shihezi University, 221st Beisi Road, Shihezi 832002, China.
Key Laboratory for Green Processing of Chemical Engineering of Xinjiang Production and Construction Group, School of Chemistry and Chemical Engineering, 221st Beisi Road, Shihezi 832003, China.
Molecules. 2018 Jun 18;23(6):1473. doi: 10.3390/molecules23061473.
For the first time, a novel series of tschimganin analogs were designed, synthesized, and evaluated for their insecticidal and fungicidal activities. Their structures were characterized by ¹H-NMR, C-NMR and HRMS. Some of these compounds displayed excellent insecticidal and fungicidal activities, suggesting that they have potential to be used as bifunctional agrochemicals. Compound and with electron donating groups showed better inhibitory activity and growth inhibition activity towards (Hübner). The properties and positions of the substituents on the benzene ring have an important influence on the acaricidal activity of tschimganin analogs. Topomer comparative molecular field analysis (CoMFA) was employed to develop a three-dimensional quantitative structure-activity relationship model for the compounds against Ugarov et Nikolski. It was indicated that higher electronegativity was beneficial for acaricidal activity. Moreover, compound having a 2-hydroxy-3,5- dinitrophenyl moiety displayed a fungicidal spectrum as broad as azoxystrobin against these phytopathogens.
首次设计、合成了一系列新型的 tschimganin 类似物，并评价了它们的杀虫和杀菌活性。它们的结构通过 ¹H-NMR、C-NMR 和 HRMS 进行了表征。这些化合物中的一些表现出优异的杀虫和杀菌活性，表明它们有可能被用作双功能农用化学品。具有供电子基团的化合物 和 对 （Hübner）表现出更好的抑制活性和生长抑制活性。苯环上取代基的性质和位置对 tschimganin 类似物的杀螨活性有重要影响。拓扑比较分子场分析（CoMFA）被用于为化合物针对 Ugarov et Nikolski 建立三维定量构效关系模型。结果表明，较高的电负性有利于杀螨活性。此外，具有 2-羟基-3,5-二硝基苯基部分的化合物 对这些植物病原菌表现出与唑菌酯相当广谱的杀菌活性。
