Synthesis and evaluation of acetylcholinesterase inhibitory effects of 2-(2-(4-benzoylpiperazin-1-yl)ethyl)-1H-benzo[de]isoquinoline-1,3(2H)-dione derivatives with potential anti-Alzheimer activity

摘要

Alzheimer’s disease (AD) is the most common form of dementia in elderly people. The disease is characterized as age-dependent chronic and neurodegenerative disorder. Cognitive decline is supposed to be related to the degeneration of cholinergic neurons in the affected brain structures. Design and development of novel acetylcholinesterase inhibitors is one of the interesting areas in medicinal chemistry. In the current project, a new series of naphthalimide-based anti-acetylcholinesterase were synthesized and their enzyme inhibitory potency was assessed using Ellman's protocol. Fortunately, the most of tested derivatives demonstrated favorable acetylcholinesterase activity. Amongst tested derivatives, compound 4k (3-OCH3) was the most active compounds in these series (IC50 = 0.26 μM).