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Discovery of novel bicyclic and tricyclic cyclohepta[b]thiophene derivatives as multipotent AChE and BChE inhibitors, in-Vivo and in-Vitro assays, ADMET and molecular docking simulation.
Eur J Med Chem
December 2024
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Sinai University, Kantara Branch, Ismailia, 41636, Egypt.
Alzheimer's disease (AD) is primarily caused by oxidative stress, hyperphosphorylated τ-protein aggregation, and amyloid-β deposition. Changes in dopaminergic and serotoninergic neurotransmitter pathways are linked to certain symptoms of AD. Derivatives of bicyclic and tricyclic cyclohepta[b]thiophene were developed to identify new potential candidates as acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitors for the treatment of AD.
View Article and Find Full Text PDFDeoxyvasicinone hybrids in the management of Alzheimer's disease: Recent advances on manmade derivatives, pharmacological activities, and structure-activity relationship.
Arch Pharm (Weinheim)
January 2025
Department of Pharmacognosy, University Institute of Pharma Sciences, Chandigarh University, Mohali, Punjab, India.
Alzheimer's disease (AD) is a prevalent neurological illness that affects over 80% of aged adults globally in cases of dementia. Although the exact pathophysiological causes of AD remain unclear, its pathogenesis is primarily driven by several distinct biochemical alterations: (i) the accumulation of toxic Aβ plaques, (ii) the hyperphosphorylation of tau proteins, (iii) oxidative stress resulting in cell death, and (iv) an imbalance between the two main neurotransmitters, glutamate and acetylcholine (ACh). Currently, there are very few medications available and no treatment.
View Article and Find Full Text PDFEfficacy of Donepezil for Fatigue and Psychological Symptoms in Post-COVID-19 Condition: Study Protocol for a Multicenter Randomized, Placebo-controlled, Double-blind Trial.
Ann Clin Epidemiol
October 2024
Department of Emergency and Critical Care Medicine, St. Marianna University School of Medicine, Kanagawa, Japan.
Background: Approximately 30% of coronavirus disease 2019 COVID-19 patients develop fatigue and psychological symptoms. We previously demonstrated the efficacy of donepezil, an acetylcholinesterase inhibitor that is widely used to treat dementia, in basic research.
Methods: This is a multicenter, double-blind, randomized, controlled, phase II clinical trial in which 120 patients with COVID-19 will be randomized in a 1:1 ratio to a donepezil or placebo group.
Current Updates on Nanotechnology-based Drug Delivery Platforms for Treating Alzheimer's with Herbal Drugs.
Pharm Nanotechnol
December 2024
Institute for Medical Research, University of Sharjah, Sharjah United Arab Emirates.
Alzheimer's disease (AD) is an irreversible brain disorder that led to memory loss and disrupts daily life. Earlier strategies to treat AD such as acetylcholinesterase inhibitor (AChEI) drugs are not showing effectiveness due to the inability to cross the blood-brain barrier. Moreover, traditional AChEI provides limited efficacy in terms of bioavailability and solubility for treating AD treatment.
View Article and Find Full Text PDFUse of Cholinesterase Inhibitors for Treatment and Prevention of Cognitive Adverse Effects of Electroconvulsive Therapy: A Systematic Review.
J ECT
December 2024
Pharmacy Service, Durham VA Health Care System, Durham, NC.
Although electroconvulsive therapy (ECT) is effective for treating depression, schizophrenia, and mania, cognitive adverse effects may limit use. One possible mechanism for these effects includes cholinergic transmission alterations, supporting potential use of cholinesterase inhibitors for prevention and treatment of these cognitive deficits. The objective of this review is to determine efficacy and safety of cholinesterase inhibitors clinically used for dementia in reducing ECT cognitive adverse effects.
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