【摘要】 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%.更多还原

【Abstract】 According to our previous research on the antiviral activity of β-carboline and tetrahydro-β-carboline derivatives,series of novel tetrahydro-β-carboline derivatives containing acylhydrazone moiety and different substituents at 1 position were designed,synthesized via Pictet-Spengler reaction,and evaluated for their biological activities.Most of these compounds exhibited excellent antiviral activity both in vitro and in vivo.The in vivo inactivation,curative,and protection activities of part of these compounds were much higher than that of ribavirin(36.5%,35.2%,and 37.1%at500 μg/mL) and harmine(40.5%,38.6%and 42.4%at 500 μg/mL).Especially,the in vivo activities of compounds Ⅵ-1(61.4%,57.2%,and 68.1%) and compound Ⅵ-2(74.5%,69.0%,and 68.1%) at 500 μg/mL,which were nearly twofold of that of ribavirin at 500 μg/mL.At the same time,the fungicidal results showed that compound Ⅳ-2 exhibited more than 60%fungicidal activities against 5 kinds of phytopathogens.Additionally,compound Ⅳ-5 exhibited more than60%larvicidal activity against C.pipiens pallens at 0.25 mg/kg.更多还原