Safety and efficacy of acetylcholinesterase inhibitors for Alzheimer's disease: A systematic review and meta-analysis
Adv Clin Exp Med. 2024 Mar 1. doi: 10.17219/acem/176051. Online ahead of print.ABSTRACTAlzheimer's disease (AD) affects millions of people worldwide. The most commonly used drugs are acetylcholinesterase inhibitors, i.e., donepezil, galantamine and rivastigmine, which increase levels of acetylcholine. However, the exact efficacy and safety of acetylcholinesterase inhibitors in the treatment of AD is still unclear. The main objective of the current study was to determine the exact safety and efficacy profile of acetylcholinesterase inhibitors in the treatment of AD by conducting a systematic review and meta-analysis of clin...
Source: Adv Data - March 5, 2024 Category: Epidemiology Authors: Yaqi Gao Yulin Liu Yanfang Li Source Type: research
Insights on synthetic strategies and structure-activity relationship of donepezil and its derivatives
AbstractThis comprehensive review focuses on the synthesis and derivatives of donepezil, a pivotal Alzheimer ’s disease (AD) medication introduced in 1997. As a selective acetylcholinesterase inhibitor with 100% oral bioavailability and a 70-h half-life, donepezil’s success in neurodegenerative disorder management has spurred extensive research into its synthesis and structural modifications. The revie w examines diverse synthetic approaches, evaluating their efficiency, cost, toxicity, and scalability. Methods range from traditional hazardous chemicals to eco-friendly strategies. Structural modifications and their imp...
Source: Medicinal Chemistry Research - March 1, 2024 Category: Chemistry Source Type: research
Hybrid pharmacophore design and synthesis of donepezil-inspired aurone derivative salts as multifunctional acetylcholinesterase inhibitors
The objective of this study was to design and synthesize valuable agents derived from flavonoids for relieving the symptoms of AD. A variety of flavonoid derivative salts incorporating benzylpyridinium units were synthesized and several of them remarkedly inhibited acetylcholinesterase (AChE) activity in vitro. Additionally, aurone derivative salts protected against cell death resulting from t-BHP exposure in rat pheochromocytoma PC12 cells and slightly promoted neurite outgrowth. Furthermore, they potently suppressed the aggregation of amyloid-β (Aβ1-42). Our findings highlight the effectiveness of donepezil-inspired au...
Source: Bioorganic Chemistry - February 24, 2024 Category: Chemistry Authors: Rei Funahashi Fumiaki Matsuura Masayuki Ninomiya Sayo Okabe Shigeo Takashima Kaori Tanaka Atsuyoshi Nishina Mamoru Koketsu Source Type: research
< em > In Silico < /em > Investigation of Novel Compounds as Inhibitors of Acetylcholinesterase Enzyme for the Treatment of Alzheimer's Diseases
Int J Alzheimers Dis. 2024 Feb 8;2024:2988685. doi: 10.1155/2024/2988685. eCollection 2024.ABSTRACTAlzheimer's disease (AD) is a "progressive, neurodegenerative disease that occurs when nerve cells in the brain die." There are only 4 drugs approved by the United States Food and Drug Administration (FDA). Three (donepezil, rivastigmine, and galantamine) out of these four drugs are anticholinesterase inhibitors, while the fourth one memantine is an N-methyl-D-aspartate (NMDA) receptor inhibitor. Currently, two immunotherapy drugs that target amyloid protein (donanemab and lecanemab) are being considered for the treatment of ...
Source: International Journal of Alzheimers Disease - February 19, 2024 Category: Geriatrics Authors: Kassim Adebambo Oghenekevwe Claudia Ojoh Source Type: research
