What are the key findings regarding the multifunctional properties of rivastigmine hybrids in the context of Alzheimer's disease (AD) therapy?

Label:chem

Topic
Alzheimer's disease (AD) is a multifactorial neurodegenerative disorder characterized by the accumulation of amyloid-β (Aβ) plaques, oxidative stress, and cholinergic deficits. Current therapies targeting single factors have shown limited efficacy, prompting the development of multi-target drugs (MTDs) that can address multiple pathological processes simultaneously.
Answer
A study designed and synthesized a series of rivastigmine hybrids incorporating antioxidant motifs. These hybrids demonstrated significant antioxidant activity, inhibitory effects on cholinesterases (AChE and BChE), and the ability to inhibit Aβ1–42 aggregation. The best multifunctional capacity was observed in the caffeic acid derivatives (4AY5 and 4AY6), while the Trolox derivatives (4AY2 and 4BY2) showed the best neuroprotective activity against oxidative damage. Molecular docking studies provided insights into the binding modes of these hybrids to cholinesterases, highlighting key interactions despite some lack of correlation with inhibitory potency.
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