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Donepezil: A review of the recent structural modifications and their impact on anti-Alzheimer activity BJPS
Mohsin,Noor ul Amin; Ahmad,Matloob.
Alzheimer disease (AD) is characterized by a low level of acetylcholine, beta-amyloid (Aβ) aggregation and oxidative stress. Donepezil is the core medicine used for the treatment of AD. Various structural modifications of donepezil have been carried out. Benzylpiperidine part of donepezil has been replaced with benzylpyridine, pyridyl methylpiperidine, benzylpiperazine, pyrimidyl piperazine. These derived molecules showed promising activities as anti-Alzheimer agents. Replacement of indanone part by other heterocyclic rings such as pyridine resulted in the formation of compounds which exhibited monoamine oxidase (MAO) as well as acetylcholinesterase (AChE) inhibition. Propargylamine containing derivatives displayed AChE as well as MAO inhibition...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Acetylcholinesterase (AChE); Butyrylcholinesterase (BuChE); Benzylpiperidine; Indanone; Hybrid compounds.
Ano: 2020 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502020000100702
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Synthesis and DPPH scavenging assay of reserpine analogues, computational studies and in silico docking studies in AChE and BChE responsible for Alzheimer's disease BJPS
Yar,Muhammad; Arshad,Muhammad; Farooq,Ariba; Gilani,Mazhar Amjad; Ayub,Khurshid; Ejaz,Asma; Kumar,Anupriya; Ninomiya,Ichiya.
Alzheimer's disease (AD) is a fast growing neurodegenerative disorder of the central nervous system and anti-oxidants can be used to help suppress the oxidative stress caused by the free radicals that are responsible for AD. A series of selected synthetic indole derivatives were biologically evaluated to identify potent new antioxidants. Most of the evaluated compounds showed significant to modest antioxidant properties (IC50 value 399.07 140.0±50 µM). Density Functional Theory (DFT) studies were carried out on the compounds and their corresponding free radicals. Differences in the energy of the parent compounds and their corresponding free radicals provided a good justification for the trend found in their IC50 values. In silico, docking of compounds into...
Tipo: Info:eu-repo/semantics/article Palavras-chave: Alzheimer's disease; Antioxidant compounds; Chronic diseases; Density Functional Theory; Molecular docking; Computational studies; DPPH assay; Indole derivatives; Acetylcholinesterase (AChE); Butyrylcholinesterase (BChE).
Ano: 2015 URL: http://www.scielo.br/scielo.php?script=sci_arttext&pid=S1984-82502015000100053
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