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本文基于天然噻唑生物碱1设计合成了一系列噻唑酰胺衍生物,采用氢谱(~1H NMR)、碳谱(~(13)C NMR)、高分辨质谱(HRMS)对所合成化合物进行了表征,并研究了它们对有害藻铜绿微囊藻(Microcysis aeruginosa)和斜生栅藻(Scenedesmus Obliquus)抑制活性,初步总结了其结构与活性的关系.活性数据表明,大部分化合物表现出比天然噻唑生物碱1更高的杀藻活性.初步结构与活性关系研究表明,噻唑酰胺是该类化合物杀藻活性中心,苯环与芳杂环直接结合噻唑酰胺可以提高活性.化合物TM7对斜生栅藻半抑制浓度(IC_(50))达到0.45 mg/L,表现出很高的抑制活性,明显优于对照药剂CuSO_4和敌草隆,展示出良好的研究潜力.
In this paper, a series of thiazole amide derivatives were designed and synthesized based on natural thiazole alkaloid 1. The synthesized compounds were characterized by 1H ~ 1H NMR, ~ 13 C NMR and HRMS. , And their inhibitory activity against the harmful algae Microcysis aeruginosa and Scenedesmus obliquus were studied and the relationship between their structure and activity was preliminary summarized.The activity data showed that most of the compounds showed a higher activity than the natural thiazoles Alkaloids 1 higher algae activity.Studies on the relationship between the initial structure and activity of thiazoleamide is the algicidal activity of these compounds center, benzene ring and aromatic heterocyclic ring directly combined with thiazole amide can increase activity.Compound TM7 of Stachys algae The half inhibitory concentration (IC 50) reached 0.45 mg / L, showing a high inhibitory activity, which was significantly better than the control agents CuSO 4 and Diuron, showing good research potential.