论文部分内容阅读
基于前期工作中对于β-咔啉和四氢-β-咔啉类化合物的抗烟草花叶病毒活性的研究,我们利用Pictet-Spengler反应设计和合成了含有酰腙结构的四氢-β-咔啉类衍生物,并对该类化合物的生物活性进行了研究,重点研究1位取代基的改变对化合物活性的影响.研究发现大部分化合物表现优异的抗烟草花叶病毒离体和活体活性.在500μg/mL浓度下,部分化合物的抗烟草花叶病毒活体活性(活体钝化、活体治疗、活体保护)明显高于商品化品种病毒唑(36.5%、35.2%和37.1%)和β-咔啉生物碱harmine(40.5%、38.6%和42.4%),尤其是化合物Ⅳ-1(61.4%、57.2%和68.1%,500μg/mL)和Ⅳ-2(74.5%、69%和68.1%,500μg/mL)的活性水平接近病毒唑的两倍.在杀菌方面,化合物Ⅳ-2在50 mg/kg的浓度下对5种菌的杀菌活性大于60%.在杀虫方面,化合物Ⅳ-5在0.25 mg/kg的浓度下对蚊幼虫的杀虫活性大于60%.
Based on the previous work on anti-tobacco mosaic virus activity of β-carbolines and tetrahydro-β-carbolines, we designed and synthesized a tetrahydro-β-carbazole containing acylhydrazone structure by Pictet-Spengler reaction And the biological activities of these compounds have been studied, focusing on the impact of the 1 substituent on the activity of the compounds.It has been found that most of the compounds exhibit excellent anti-tobacco mosaic virus activity in vitro and in vivo. The anti-tobacco mosaic virus activity of some compounds (in vivo passivation, in vivo treatment, in vivo protection) was significantly higher than that of the commercial varieties ribavirin (36.5%, 35.2% and 37.1%) and β-carbazole at 500μg / mL The morpholine alkaloids harmine (40.5%, 38.6% and 42.4%), especially compounds IV-1 (61.4%, 57.2% and 68.1%, 500μg / mL) and IV-2 (74.5%, 69% and 68.1%, 500μg / mL) was close to twice the activity of ribavirin.In the case of bactericidal activity, compound IV-2 had a bactericidal activity of more than 60% against five bacteria at a concentration of 50 mg / kg.Compound IV-5 Insecticidal activity against mosquito larvae is greater than 60% at a concentration of 0.25 mg / kg.