Design, Synthesis, and Biological Activity of Donepezil: Aromatic Amine Hybrids as Anti-Alzheimerss Drugs.

ABSTRACT: In this study, benzylpiperidine, the active group of donepezil (DNP), was connected with the neurotransmitter phenylethylamine by square amide, in which the fat chain of phenylethylamine was reduced and the benzene rings were substituted. A series of multifunctional hybrid compounds, including DNP-aniline hybrids (1-8), DNP-benzylamine hybrids (9-14), and DNP-phenylethylamine hybrids (15-21) were obtained and their cholinesterase inhibitory activity and neuroprotection of the SH-SY5Y cell line were determined. Results showed that compound 3 exhibited excellent acetylcholinesterase inhibitory activity with an IC₅₀ value of 4.4 μM, higher than that of positive control DNP and significant neuroprotective effects against H₂O₂-induced

SUBMITTER: Wan D 

PROVIDER: S-EPMC10286275 | biostudies-literature | 2023 Jun

REPOSITORIES: biostudies-literature