Individuals with Alzheimer's disease (AD), one of the most common causes of dementia, display serious neurological deficits characterized by the decrease in various cognitive functions. The cause of AD is yet to be determined, but reversible inhibitors of acetylcholinesterase (AChE) have been shown to improve cognitive function in individuals with AD. The synthesis of new, multifunctional inhibitors for AChE is the necessary basis to be able to design better functioning AD medications. Two different pterostilbene amino alcohol derivatives were synthesized, as similar compounds have been shown to be reversible inhibitors specific to AChE. In addition to its inhibitory ability, the antioxidant activity of pterostilbene has a neuroprotective effect against H2O2 and reactive oxygen species induced cell damage. Depending on the added secondary amine, some compounds also show potential inhibitory activity on the self-induced aggregation of amyloid β1-42, a protein fragment widely found in the brains of individuals with AD. The inhibitory and antioxidant activity of the pterostilbene derivatives were evaluated in ORAC-FL and inhibition assays. The data suggest that the synthesized compounds could be multifunctional inhibitors for AChE, making them a possible starting point for the development of new AD medications.

Synthesis and evaluation of pterostilbene amino alcohol derivatives as antioxidants and reversible acetylcholinesterase inhibitors

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