6-(哌嗪-1-基)-去氢骆驼蓬碱酰胺衍生物的合成及抑菌活性

Synthesis and antifungal activity of 6-(piperazin-1-yl)-harmine amide derivatives

摘要: 为探索6-(哌嗪-1-基)-去氢骆驼蓬碱酰胺衍生物的抑菌活性, 结合前期的衍生化研究, 设计并合成了 15 个新型6-(哌嗪-1-基)-去氢骆驼蓬碱衍生物, 并对其抑菌活性及构效关系进行了研究。离体抑菌活性测定结果表明, 目标化合物在 50 μg/mL 下对番茄灰霉病菌Botrytis cinerea、小麦赤霉病菌Fusarium graminearum、梨树腐烂病菌Valsa pyri、棉花枯萎病菌Fusarium oxysporum均有一定的抑制活性，尤其化合物 5j 对棉花枯萎病菌表现出较好的活性，抑制率达61.7%，强于阳性对照啶酰菌胺。

Abstract: In order to explore the antifungal activity of 6-(piperazin-1-yl)-harmine amide derivative, based on previous derivative studies, 15 novel 6-(piperazin-1-yl)-harmine derivatives were designed and synthesized. The antifungal activity was evaluated and the structure-activity relationship was analyzed. The in vitro bioassay results demonstrated that the target compounds showed antifungal activities against Botrytis cinerea, Fusarium graminearum, Valsa pyri and Fusarium oxysporum, especially compound 5j displayed excellent activity against F. oxysporum with inhibition rate of 61.7% at 50 μg/mL, which was better than the positive control boscalid.