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- Title
Pityriacitrin marine alkaloids as novel antiviral and anti‐phytopathogenic‐fungus agents.
- Authors
Wang, Tie‐Nan; Yang, Shan; Shi, Shao‐Yang; Yuan, Wen‐Ying; Chen, Jian‐Xin; Duan, Zhong‐Yu; Lu, Ai‐Dang; Wang, Zi‐Wen; Wang, Qing‐Min
- Abstract
BACKGROUND: Plant diseases have been gripping agricultural production, seriously affecting the growth and yields of crops. Marine natural products are an important source for novel drugs discovery. In this work, pityriacitrin marine alkaloids were selected as the parent structures. A series of pityriacitrin alkaloid analogues were rationally designed, synthesized and evaluated for their antiviral activities and fungicidal activities. RESULT: Most of these compounds were demonstrated to have higher antiviral activities than ribavirin. Particularly, compounds 3a, 3e, 8f, 8g, and 9g displayed higher anti‐TMV activities than ningnanmycin at 500 μg·mL−1. Mechanism research revealed that 3a could bind to TMV CP with an excellent affinity (Ka = 8.67 × 106 L·mol−1), thus interfere with the assembly of virus particles. These alkaloids also showed broad‐spectrum fungicidal activities against eight kinds of phytopathogenic fungi. Compound 5f with 1.43–3.84 μg·mL−1 EC50 value against three fungi emerged as a new fungicidal candidate. CONCLUSION: Pityriacitrin alkaloids and their derivatives were synthesized and evaluated for anti‐TMV and fungicidal activities for the first time. Compounds 3a and 5f with excellent activities emerged as new candidates for antiviral research and fungicidal research, respectively. Current work provided a new idea for the molecular design and development of novel plant virus and fungi inhibitors in the future. © 2021 Society of Chemical Industry.
- Subjects
SOCIETY of Chemical Industry (Great Britain); ALKALOIDS; MARINE natural products; ANTIVIRAL agents; PLANT viruses; PHYTOPATHOGENIC fungi; RIBAVIRIN
- Publication
Pest Management Science, 2021, Vol 77, Issue 10, p4691
- ISSN
1526-498X
- Publication type
Article
- DOI
10.1002/ps.6510