An economical new process has been developed for the synthesis of donepezil hydrochloride (1) an anti-Alzheimer's drug. The process involves Darzen reaction of pyridine-4-carboxaldehyde and 2-bromo-5,6-dimethoxy indanone affording epoxide 5,6-dimethoxy-3-(pyridine-4-yl)spiro[indene-2,2'-oxiran]-1(3H)-one (4) as a key intermediate. The one-pot deoxygenation of 4 and hydrogenation of the aryl moiety in high yield improved the overall yield of the process.
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http://dx.doi.org/10.1248/cpb.58.1157 | DOI Listing |
Background: Senile dementia (SD) is a deteriorative organic brain disorder and it comprises Alzheimer's disease (AD) as a major variant. SD is shown impairment of mental capacities whereas AD is degeneration of neurons. According to World Health Organization (WHO) report; more than 55 million peoples have dementia and it is raising 10 million new cases every year.
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December 2024
Afe Babalola University, Ado-Ekiti (ABUAD), Ado-Ekiti, Ekiti state, Nigeria.
Background: The impact of probiotics as gut and immunological modulator in restoring gut microbial balance and immune cells expression have generated much attention in the health sector. Its inhibitory effect on bacterial translocation and associated neural inflammatory processes has been reported. However, there is scarcity of data on its neuroprotective impact against neuroinflammation-associated neurodegeneration and memory impairment.
View Article and Find Full Text PDFAlzheimers Dement
December 2024
STEM Neurology & Neuropsychological0 Research Group Egypt (SNRGE), Port Said, Port Said, Egypt.
Background: Donepezil, an acetylcholinesterase inhibitor (AChEI), is an FDA-approved drug to treat these neurodegenerative diseases, e.g., Alzheimer's Disease (AD) and Mild Cognitive Impairment (MCI).
View Article and Find Full Text PDFAlzheimers Dement
December 2024
Chitkara College of Pharmacy, Chitkara University, Rajpura, Punjab, India.
Background: The present study recapitulates the potency of the novel synthesized piperazine-benzoquinone derivative as a lead molecule selectively targeting AChE along with the antioxidative potential for the management of cognitive decline in Alzheimer's disease.
Method: Novel piperazine-benzoquinone derivative was synthesized implementing appropriate synthetic procedures and was characterized by various spectral and elemental techniques. The purity of this synthetic analogue was ascertained by TLC, melting point determination and elemental analyses.
Alzheimers Dement
December 2024
HealthPartners Institute, Minneapolis, MN, USA.
Background: Cholinesterase inhibitors (ChEIs) are cornerstones in the symptomatic treatment of Alzheimer's disease (AD) and dementia with Lewy bodies (DLB) and are also prescribed for vascular dementia (VD). Despite their widespread use, patterns of prescribing ChEIs are not fully understood.
Objective: Examine the prevalence, timing, and types of ChEI prescriptions before and after dementia diagnosis including prescribing patterns by patient sex and race.
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