Discovery of glyantrypine‐family alkaloids as novel antiviral and antiphytopathogenic‐fungus agents

作者：Yanan Hao, Mo Yu, Kaihua Wang, Binbing Zhu, Ziwen Wang, Yuxiu Liu, Dejun Ma, Qingmin Wang · 发表于：Pest Management Science · 年份：2021 · DOI：10.1002/ps.6709 · 被引用次数：10 · 研究领域：Chemical synthesis and alkaloids、Berberine and alkaloids research、Fungal Plant Pathogen Control

BACKGROUND: Plant diseases caused by viruses and fungi have caused great losses to crop quality and yield. The discovery of novel and efficient antiviral and antiphytopathogenic-fungus agents is urgently needed. It is the most important pesticide innovation strategy to find active compounds from natural products. Here, glyantrypine-family alkaloids were taken as the parent structures and a series of their derivatives were designed through molecular splicing, ring expansion, and ring contraction strategies, and synthesized. The anti-tobacco mosaic virus (TMV) activities and antifungal activities of these alkaloids were systematically investigated for the first time. RESULT: for inactivation, curative, and protection activity in vivo, respectively). Compounds 18d and 28d with good antiviral activities were selected for antiviral mode of action studies, which indicated that these alkaloids could achieve good antiviral effects by inhibiting TMV particle extension during assembly. These compounds also exhibited broad-spectrum fungicidal activities. CONCLUSION: Glyantrypine-family alkaloids and their derivatives were synthesized and evaluated for anti-TMV and fungicidal activities for the first time. Compounds 18d and 28d with excellent antiviral activities and compound 7bc with remarkable fungicidal activity emerged as novel lead compounds. This study lays a foundation for the application of glyantrypine alkaloids in plant protection.