A new napthalene derivative with anti-amyloidogenic activity as potential therapeutic agent for alzheimer's disease

2020 
Abstract Alzheimer's disease (AD) is a highly prevalent neurodegenerative disorder that primarily affects the elderly population worldwide. One of several theories explaining the pathophysiology of AD relates to β-amyloid aggregates, which have emerged as the main cause of synaptic loss and neurodegeneration in AD patients. Previous research has shown that β-amyloids comprise a wide spectrum of species, including monomers, oligomers and fibrils. While the physiological role of β-amyloid monomers has been highlighted, oligomers and fibrils appear to be the main contributors to neurotoxicity in AD. Consequently, a therapeutic approach to the disease should include the inhibition of both oligomerisation and the fibrillation process. This paper outlines the synthesis of new naphthalene derivatives, as well as their in silico, in vitro and in vivo evaluations of their properties as anti-β-amyloidogenic agents. Molecular dynamic simulations predicted the formation of thermodynamically stable (ΔG
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