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。
[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.
出处
《农药》
CAS
CSCD
北大核心
2018年第1期3-6,共4页
Agrochemicals
基金
新疆维吾尔自治区研究生科研创新项目(XJGRI2016052)
