Abstract
Alzheimer's disease (AD) is a progressive neurological degenerative disease that has complex pathogenesis. A variety of studies in humans indicate that several enzymes inhibitors can be useful in the treatment of AD, including acetylcholinesterase (AchE), butyrylcholinesterase (BuChE) and monoamine oxidase (MAO). Various substituted 4-arylcoumarin derivatives were synthesised, and their activity in vitro were investigated, including AChE/BuChE inhibitory activity, MAO inhibitory activity, and antioxidant activity. Most of the compounds were found to exhibit high inhibitory activity, and individual compounds have extremely excellent activities. Therefore 4-arylcoumarins provides an idea for drugs design for the development of therapeutic or preventive agents for AD.
Highlights
Alzheimer’s disease (AD) has become one of the major diseases that threatening the health of elder people in modern society
The most currently available drug therapies were based on the cholinergic hypothesis, which proposes that AD is caused by reduced synthesis of the neurotransmitter acetylcholine (ACh)[2]
The results showed that 3-arylcoumarins with a R5, R6-dihydroxy group has a significantly stronger inhibitory activity than the R6- or R5-position mono-substituted
Summary
Alzheimer’s disease (AD) has become one of the major diseases that threatening the health of elder people in modern society. AD is a refractory disease with complicated etiopathogenesis Several hypotheses, such as cholinergic hypothesis, were proposed to explain the cause of the disease. Patil et al.[21] reviewed the synthesis and designed aspects of coumarin derivatives as MAO inhibitors for AD, in which most 3-arylcoumarin compounds selectively inhibit MAO-B and give some guidance in modifying the structure. Previous studies[15,21,22,23,24] have designed coumarin derivatives as potential inhibitors of MAO and ChE, and have achieved good results.
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