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Design, synthesis and antifungal activity evaluation of isocryptolepine derivatives

文献类型： 外文期刊

作者： Li, Jun-cai 1 ; Wang, Ren-xuan 1 ; Sun, Yu 1 ; Zhu, Jia-kai 1 ; Hu, Guan-fang 2 ; Wang, Yu-ling 2 ; Zhou, Rui 1 ; Zhao, Z 1 ;

作者机构： 1.Lanzhou Univ, Sch Pharm, Lanzhou 730000, Gansu, Peoples R China

2.Gansu Acad Agr Sci, Inst Plant Protect, Lanzhou 730070, Gansu, Peoples R China

关键词： Isocryptolepine; Antifungal activity; Structure-activity relationship; Mode of action

期刊名称：BIOORGANIC CHEMISTRY （ 影响因子：5.275； 五年影响因子：5.252 ）

ISSN： 0045-2068

年卷期： 2019 年 92 卷

页码：

收录情况： SCI

摘要： In this paper, the nitrogen atom was inserted into the anthracycline system of the isocryptolepine nucleus to obtain the "Aza"-type structure benzo[4,5]imidazo [1,2-c] quinazoline. A series of "Aza"-type derivatives were designed, synthesized and evaluated for their antifungal activity against six plant fungi in vitro. Among all derivatives, compounds A-0, B-1 and B-2 showed significant antifungal activity against B. cinerea with the EC50) values of 2.72 mu g/mL, 5.90 mu g/mL and 4.00 mu g/mL, respectively. Compound A-2 had the highest activity against M. oryzae with the EC50) values of 8.81 mu g/mL, and compound A-1 demonstrated the most control efficacy against R. solani (EC50, 6.27 mu g/mL). Moreover, compound A-0 was selected to investigate the in vivo tests against B. cinerea and the results indicated that the preventative efficacy of it up to 72.80% at 100 mu g/mL. Preliminary mechanism studies revealed that after treatment with A-0 at 5 mu g/mL, the B. cinerea mycelia appeared curved, collapsed and the cell membrane integrity may be damaged. The reactive oxygen species production, mitochondrial membrane potential and nuclear morphometry of mycelia have been changed, and the membrane function and cell proliferation of mycelia were destroyed. Compounds A-0, A-1, B-1 and B-2 presented weaker toxicities against two cells lines than isocryptolepine. This study lays the foundation for the future development of isocryptolepine derivatives as environmentally friendly and safe agricultural fungicides.

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