作者
Muhammed Alzweiri, Amsha S Alsegiani, Endri Karaj, Daniyah A Almarghalani, Yahia Tabaza, Zahoor A Shah, LM Viranga Tillekeratne
发表日期
2021/9/1
期刊
Bioorganic & medicinal chemistry letters
卷号
47
页码范围
128205
出版商
Pergamon
简介
Alzheimer’s disease (AD) is a neurodegenerative disorder, projected to be the second leading cause of mortality by 2040. AD is characterized by a progressive impairment of memory leading to dementia and loss of ability to carry out daily functions. In addition to the deficiency of acetylcholine release in synapse, there are other mechanisms explaining the etiology of the disease. The most disputing ones are associated with the accumulation of damaged proteins β-amyloid (Aβ) and hyperphosphorylated tau outside and inside neurons, respectively. Lysergic acid derivatives have been shown to possess promising anti-Alzheimer effect. Moreover, lysergic acid structure encompasses the general structural requirements for acetylcholinesterase inhibition. In this study, sixteen analogues, derived from lysergic acid structure, were synthesized. Heck and Mannich reactions were carried out to 4-bromo indole nucleus to …
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M Alzweiri, AS Alsegiani, E Karaj, DA Almarghalani… - Bioorganic & medicinal chemistry letters, 2021