Aminoalkyl-substituted flavonoids: synthesis, cholinesterase inhibition, β-amyloid aggregation, and neuroprotective study

AbstractIn this manuscript, 17 aminoalkyl-substituted flavonoid derivatives were synthesized and their anticholinesterase, anti-beta-amyloid (A β) aggregation and neuroprotective activities were evaluated. The synthesized compounds were prepared through four-step reaction, started from the reaction between 2-hydroxyacetophenone and 4-methoxy benzaldehyde. Among the final compounds,6j displayed the best anti-butyrylcholinesterase activity (IC50 = 0.335 μM). Moreover, compound6i significantly protected PC12 neurons against H2O2-induced cell death. This compound could also inhibit acetylcholinesterase and self-induced A β peptide aggregation by 51.3% and 49.2%, respectively. The results indicated that compound6i could be considered as a lead compound towards the discovery of disease-modifying drugs for Alzheimer ’s disease (AD) therapy.
Source: Medicinal Chemistry Research - Category: Chemistry Source Type: research