Synthesis and biological evaluation of 4-arylcoumarins as potential anti-Alzheimer's disease agents
Yinling Yun1, Jie Yang1, Yuhang Miao1
1School of Medicine and Life Sciences, University of Jinan-Shandong Academy of Medical Sciences, Jinan, Shandong, China; Institute of MateriaMedica, Shandong Academy of Medical Sciences, Jinan, Shandong, China; Key Laboratory for Biotech-Drugs Ministry of Health, Jinan, Shandong, China; Key Laboratory for Rare & Uncommon Diseases of Shandong Province, Jinan, Shandong, China.
Abstract:
Alzheimer's disease (AD) is a progressive neurological degenerative disease that has complex pathogenesis. A variety of studies in humans indicate that several enzymes inhibitors can be useful in the treatment of AD, including acetylcholinesterase (AchE), butyrylcholinesterase (BuChE) and monoamine oxidase (MAO). Various substituted 4-arylcoumarin derivatives were synthesised, and their activity in vitro were investigated, including AChE/BuChE inhibitory activity, MAO inhibitory activity, and antioxidant activity. Most of the compounds were found to exhibit high inhibitory activity, and individual compounds have extremely excellent activities. Therefore 4-arylcoumarins provides an idea for drugs design for the development of therapeutic or preventive agents for AD.
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