Structural Simplification of Marine Natural Products: Discovery of Hamacanthin Derivatives Containing Indole and Piperazinone as Novel Antiviral and Anti-phytopathogenic-fungus Agents

• DOI: 10.1021/acs.jafc.1c04098
• Publication Date: 2021-08-27T21:14:45Z
• Authors: Tienan Wang; Lin Li; Yanan Zhou; Aidang Lu; Hongyan Li; Jianxin Chen; Zhongyu Duan; Qingmin Wang
• Keywords: Natural product; Lead compound; Marine fungi

With the increasing severity of plant diseases and emergence pathogen resistance, there is an urgent need for development new efficient environment-friendly pesticides. Marine natural product (MNP) resources are rich diverse. Structural simplification based on MNPs important strategy to find novel pesticide candidates. In this work, marine 6″-debromohamacanthin A (1a) was efficiently prepared selected as parent structure. series hamacanthin derivatives were designed, synthesized, studied antiviral antifungal activities. Most these compounds displayed higher activities than ribavirin. The 1a 13e–13h similar or that ningnanmycin (perhaps most anti-plant-virus agent). Compound 13h further mechanism research via transmission electron microscopy, molecular docking, fluorescence titration. results showed compound could bind TMV CP interfere with assembly process RNA. addition, also exhibited broad-spectrum inhibitory effects against eight common agricultural pathogens. Compounds 1a, 12b, 12f excellent fungicidal can be considered candidates research. These provide a basis application alkaloids in crop protection.