新型5-脂肪基-1,2,4-三唑曼尼希碱的合成及生物活性

doi:10.11944/j.issn.1000-0518.2016.05.150267

摘要/Abstract

摘要：

设计并合成了22个具有长脂肪链取代的新型三唑曼尼希碱,研究了其植物生长调节活性、除草活性和对细胞周期分裂蛋白25B(CDC25B)抑制活性,结果发现,多数目标分子表现出优良的促进细胞生长素活性和除草活性,表明该类分子有望成为优良的新型农药;对CDC25B抑制活性筛选发现一种曼尼希碱具有优良的CDC25B抑制活性,其IC₅₀值低于阳性参照物正钒酸钠,有望成为肿瘤治疗的药物先导物。

关键词: 脂肪基-三唑, 曼尼希碱, 植物生长调节, 除草, 细胞周期分裂蛋白25B抑制剂

Abstract:

Twenty-two novel Mannich bases of 5-alkyl-1,2,4-triazole were designed and synthesized to evaluate their biological activities. The plant growth regulating activity, herbicidal activity and the inhibitory activity on cell division cycle protein 25B(CDC25B) of those molecules were screened. Most of the molecules exhibit good cytokinin activity and herbicidal activity, indicating their potential as novel pesticide. One of these molecules performs good inhibitory activity against CDC25B, and is a potential leading compound for anti-concer drug design.

Key words: alkyl-triazole, Mannich base, plant growth regulator, herbicidal activity, inhibitors against CDC25B

张成路, 程安琪, 唐杰, 国阳, 孙丽杰, 袭焕. 新型5-脂肪基-1,2,4-三唑曼尼希碱的合成及生物活性[J]. 应用化学, 2016, 33(5): 554-564.

ZHANG Chenglu, CHENG Anqi, TANG Jie, GUO Yang, XI Huan. Synthesis and Biological Activity of the Novel Mannich Bases of 5-Alkyl-1,2,4-triazole[J]. Chinese Journal of Applied Chemistry, 2016, 33(5): 554-564.

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