含吡唑环的1,2,4-三唑希夫碱类衍生物的合成及生物活性

以自制的4-氨基-4,5-二氢-3-(3,5-二甲基吡唑-1-基)甲基]-1,2,4-三唑-5-硫酮衍生物为中间体, 与取代苯甲醛反应合成了一系列新型含吡唑环的1,2,4-三唑希夫碱衍生物. 通过红外光谱、 核磁共振波谱、 高分辨质谱、 元素分析及X射线单晶衍射对目标化合物进行了结构表征, 并初步测试了其生物活性. 结果表明, 大部分化合物表现出较好的抑菌活性, 其中化合物G9, G10和G15的抑菌效果优于对照药三唑酮.

Synthesis and Biological Activities of 1,2,4-Triazole Schiff Bases Containing Pyrazole Rings†

An important class of compounds formed by 1,2,4-triazole and its derivatives were reported to exhibit a broad spectrum of biological activities. And pyrazole derivatives usually have antifungal, anticancer and herbicidal activities. The compounds containing 1,2,4-triazole and pyrazole would provide better biological activities simultaneously according biological activity of the superposition principle. In the present work, a series of novel 1,2,4-triazole Schiff bases containing pyrazole rings was synthesized by multistep reactions. Their structures were characterized by IR, ¹H NMR, ¹³C NMR, HRMS, elemental analyses and X-ray diffraction techniques. The biological activities of the target compounds for the against four vegetable pathogens containing Gibberll nicotiancola, Gibberlla saubinetii, Fusarium oxysporium f. sp. niveum and Pythium solani were evaluated. The preliminary results indicated that most of the compounds exhibit relatively good antifungal activities, especially compounds G9, G10 and G15 showed better biological activity than triazolone.