Position: Home > Articles > Synthesis and Fungicidal Activity of Novel β-Carboline Derivatives
Agrochemicals
2018
(1)
3-6
新型β-咔啉衍生物的合成与杀菌活性
作 者：
霍新玉;郭亮;韦玥婷;张洁;韩小强
单 位：
石河子大学化学化工学院新疆兵团化工绿色过程重点实验室;石河子大学农学院新疆绿洲农业病虫害治理与植保资源利用自治区高校重点实验室
关键词：
去氢骆驼蓬碱;β-咔啉;合成;抑菌活性
摘 要：
[目的]寻找具有较高生物活性的β-咔啉类农药先导化合物。[方法]以去氢骆驼蓬碱为原料,经过烷基化反应,合成7个去氢骆驼蓬碱衍生物;以L-色氨酸为原料,经过Pictet-Spengler、酯化等4步反应,合成6个β-咔啉衍生物,并对13个目标化合物进行抑菌活性测定。[结果]目标化合物结构通过核磁共振氢谱、碳谱、红外及质谱确证。初步活性测定结果表明:在质量浓度为50 mg/L条件下,目标化合物对供试的7种病原菌均表现出一定的抑制活性,其中化合物2d对梨黑斑病原菌和油菜菌核病原菌的抑制率分别为86.3%和91.19%,表现出比对照药剂啶酰菌胺优异(60.14%)和相当(91.95%)的活性。[结论]目标化合物可作为先导化合物进一步研究,为新型绿色杀菌剂研发提供理论指导。
译 名：
Synthesis and Fungicidal Activity of Novel β-Carboline Derivatives
作 者：
HUO Xin-yu;GUO Liang;WEI Yue-ting;ZHANG Jie;HAN Xiao-qiang;School of Chemistry and Chemical Engineering, Key Laboratory for Green Processing of Chemical Engineering of Xinjiang Bingtuan Shihezi University;College of Agricultural, Key Laboratory at Universities of Xinjiang Uygur Autonomous Region for Oasis Agricultural Pest Management and Plant Protection Resource Utilization Shihezi University;
关键词：
harmine;;β-carboline;;synthesis;;fungicidal activity
摘 要：
[Aims] This study aims to find agrochemical lead compounds of β-carboline with higher bioactivity.[Methods] Six harmine derivatives were synthesized from the starting material harmine by modification of 9-position ofβ-carboline nucleus, and seven β-carboline derivatives were synthesized from the starting material L-tryptophan via Pictet-Spengler condensation and followed by esterification, oxidation, hydrazine, and their antifungal activities were evaluated. [Results] The target compounds were confirmed by ~1HNMR, ~(13)CNMR, IR and MS. The preliminary results showed that most of the compounds possessed some fungicidal activity against seven phytopathogenic fungi at 50 mg/L.Compound 2 d showed higher activity(86.3%) than boscalid(60.14%) against Alternaria kikuchiana Tanaka and similar activity(91.19 %) with boscalid(91.95%) against Sclerotinia sclerotiorum(Lib.) de Bary. [Conclusions] The target compounds might be considered as lead compounds for further design and synthesis as agricultural fungicides, which provides a theoretical direction for the development of novel fugicides.
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