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Pd-Catalyzed Direct Modification of an Anti-Alzheimer’s Disease Drug: Synthesis and Biological Evaluation of α-Aryl Donepezil Analogues
- Source :
- ACS Omega, ACS Omega, Vol 6, Iss 36, Pp 23347-23354 (2021)
- Publication Year :
- 2021
- Publisher :
- American Chemical Society, 2021.
-
Abstract
- Palladium/BuAd2P efficiently catalyzed the direct α-arylation of ketone in the anti-Alzheimer's disease drug donepezil, leading to 15 aryldonepezil analogues exhibiting high selective inhibition of acetylcholinesterase (AChE). The cell-based assays revealed that the 3-methylpridinyl analogue (12) shows significantly lower toxicity compared to donepezil and remarkable neuroprotective activity against H2O2-induced damage in SH-SY5Y cells. Docking results of compound 12 also interpreted the possible mechanism of the selective inhibition between AChE and butyrylcholinesterase (BuChE).
- Subjects :
- chemistry.chemical_classification
Ketone
Aché
General Chemical Engineering
General Chemistry
Pharmacology
Acetylcholinesterase
Neuroprotection
language.human_language
Article
chemistry.chemical_compound
Chemistry
chemistry
Docking (molecular)
Toxicity
medicine
language
Donepezil
QD1-999
Butyrylcholinesterase
medicine.drug
Subjects
Details
- Language :
- English
- ISSN :
- 24701343
- Volume :
- 6
- Issue :
- 36
- Database :
- OpenAIRE
- Journal :
- ACS Omega
- Accession number :
- edsair.doi.dedup.....104efe32aceaae021ec46aa6df71ee65