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Palladium-catalyzed synthesis and acetylcholinesterase inhibitory activity evaluation of 1-arylhuperzine A derivatives.
- Source :
-
Journal of Asian natural products research [J Asian Nat Prod Res] 2023 Nov; Vol. 25 (11), pp. 1097-1109. Date of Electronic Publication: 2023 Apr 26. - Publication Year :
- 2023
-
Abstract
- A series of arylated huperzine A (HPA) derivatives ( 1 - 24 ) were efficiently synthesized in good yields (45-88% yields) through the late-stage modification of structurally complex natural anti-Alzheimer's disease (AD) drug huperzine A (HPA), using the palladium-catalyzed Suzuki-Miyaura cross-coupling reaction. The acetylcholinesterase (AChE) inhibitory activity of all synthesized compounds was evaluated to screen the potential anti-AD bioactive molecules. The results showed that introducing the aryl groups to C-1 position of HPA resulted in the unsatisfactory AChE inhibitory activity. The present study demonstrably verifies pyridone carbonyl group could be the necessary and unchangeable pharmacophore for maintaining HPA's anti-AChE potency, and provides the helpful information on the further research for developing anti-AD HPA analogues.
Details
- Language :
- English
- ISSN :
- 1477-2213
- Volume :
- 25
- Issue :
- 11
- Database :
- MEDLINE
- Journal :
- Journal of Asian natural products research
- Publication Type :
- Academic Journal
- Accession number :
- 37098899
- Full Text :
- https://doi.org/10.1080/10286020.2023.2196619