Design, synthesis, and structure–activity relationship of caffeine‐based triazoles as dual AChE and BACE‐1 inhibitors
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DOI: 10.1002/ddr.21998
Abstract: Natural products have significantly contributed to drug discovery for neurodegenerative diseases. Caffeine is one of the well‐known central nervous system(CNS)‐active natural products. Besides its CNS stimulant properties, it is a mild inhibitor of acetylcholinesterase (AChE)… read more here.
Keywords: bace; caffeine based; caffeine; ache ... See more keywords
Multitargeted C9‐substituted ester and ether derivatives of berberrubine for Alzheimer's disease: Design, synthesis, biological evaluation, metabolic stability, and pharmacokinetics
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DOI: 10.1002/ddr.22017
Abstract: Berberrubine is a naturally occurring isoquinoline alkaloid and a bioactive metabolite of berberine. Berberine exhibits a wide range of pharmacological activities, including cholinesterase inhibition. The cholinesterase inhibitors provide symptomatic treatment for Alzheimer's disease; however, multitarget‐directed… read more here.
Keywords: bace; inhibition; ester; disease ... See more keywords
Effect of sampling on BACE‐1 ligands binding free energy predictions via MM‐PBSA calculations
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DOI: 10.1002/jcc.24839
Abstract: The BACE‐1 enzyme is a prime target to find a cure to Alzheimer's disease. In this article, we used the MM‐PBSA approach to compute the binding free energies of 46 reported ligands to this enzyme.… read more here.
Keywords: bace; effect sampling; bace ligands; sampling bace ... See more keywords
The potential of natural product vs neurodegenerative disorders: In silico study of artoflavanocoumarin as BACE-1 inhibitor
Sign Up to like & getrecommendations! Published in 2018 at "Computational biology and chemistry"
DOI: 10.1016/j.compbiolchem.2018.10.015
Abstract: Increasing evidence suggests the beneficial impact of flavonoid-rich nutrition on normal cognitive function. It has been revealed that flavonoids can slow neurodegenerative processes in situations such as Alzheimer's disease (AD). The β-secretase (BACE-1) is one… read more here.
Keywords: bace; silico study; study; study artoflavanocoumarin ... See more keywords
Multipotent AChE and BACE-1 inhibitors for the treatment of Alzheimer's disease: Design, synthesis and bio-analysis of 7-amino-1,4-dihydro-2H-isoquilin-3-one derivates.
Sign Up to like & getrecommendations! Published in 2017 at "European journal of medicinal chemistry"
DOI: 10.1016/j.ejmech.2017.07.006
Abstract: In this paper, the preparation of a new class of multi-target-directed ligands (MTDLs) based on a 7-amino-1,4-dihydro-2H-isoquilin-3-one, whose lead (compound I) showed promising properties in acetylcholinesterase (AChE) inhibitory activity [1], is described. The results of… read more here.
Keywords: bace; ache; isoquilin one; amino dihydro ... See more keywords
BACE inhibitor treatment of mice induces hyperactivity in a Seizure-related gene 6 family dependent manner without altering learning and memory
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DOI: 10.1038/s41598-021-94369-0
Abstract: BACE inhibitors, which decrease BACE1 (β-secretase 1) cleavage of the amyloid precursor protein, are a potential treatment for Alzheimer’s disease. Clinical trials using BACE inhibitors have reported a lack of positive effect on patient symptoms… read more here.
Keywords: bace; treatment; family; mice ... See more keywords
BACE inhibitors in clinical development for the treatment of Alzheimer’s disease
Sign Up to like & getrecommendations! Published in 2018 at "Expert Review of Neurotherapeutics"
DOI: 10.1080/14737175.2018.1531706
Abstract: ABSTRACT Introduction: The amyloid hypothesis of Alzheimer’s disease (AD) affirms that brain accumulation of amyloid-β (Aβ) oligomers and soluble aggregates represent the major pathological event of the disease. Several anti-Aβ small organic molecules, monoclonal antibodies… read more here.
Keywords: bace; alzheimer disease; treatment; bace inhibitors ... See more keywords
Targeted BACE-1 inhibition in microglia enhances amyloid clearance and improved cognitive performance
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DOI: 10.1126/sciadv.abo3610
Abstract: Abnormal accumulation of β-amyloid (Aβ) peptides is a culprit in Alzheimer’s disease (AD); blocking Aβ generation is therefore being explored as a logical approach for AD treatment. Here, we demonstrate that targeted inhibition of β-site… read more here.
Keywords: clearance; bace; inhibition; bace microglia ... See more keywords
Beta-Site Amyloid Precursor Protein-Cleaving Enzyme Inhibition Partly Restores Sevoflurane-Induced Deficits on Synaptic Plasticity and Spine Loss
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DOI: 10.3390/ijms23126637
Abstract: Evidence indicates that inhalative anesthetics enhance the β-site amyloid precursor protein (APP)-cleaving enzyme (BACE) activity, increase amyloid beta 1-42 (Aβ1–42) aggregation, and modulate dendritic spine dynamics. However, the mechanisms of inhalative anesthetics on hippocampal dendritic… read more here.
Keywords: bace; spine density; spine; site amyloid ... See more keywords
Mangifera indica ‘Namdokmai’ Prevents Neuronal Cells from Amyloid Peptide Toxicity and Inhibits BACE-1 Activities in a Drosophila Model of Alzheimer’s Amyloidosis
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DOI: 10.3390/ph15050591
Abstract: Alzheimer’s disease (AD) is a progressive neurological illness with few effective treatments. Thus, ameliorating the effects of AD using natural products has attracted global attention with promising efficacy and safety. In this study, ten tropical… read more here.
Keywords: bace; indica namdokmai; mangifera indica; drosophila model ... See more keywords
Multitargeted Virtual Screening and Molecular Simulation of Natural Product-like Compounds against GSK3β, NMDA-Receptor, and BACE-1 for the Management of Alzheimer’s Disease
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DOI: 10.3390/ph16040622
Abstract: The complexity of Alzheimer’s disease (AD) and several side effects of currently available medication inclined us to search for a novel natural cure by targeting multiple key regulatory proteins. We initially virtually screened the natural… read more here.
Keywords: bace; f1094 0201; product like; like compounds ... See more keywords