Synthesis and biological evaluation of 4-arylcoumarins as potential anti-Alzheimer's disease agents

  • Bioorg Med Chem Lett. 2020 Feb 15;30(4):126900. doi: 10.1016/j.bmcl.2019.126900.
Yinling Yun  1 ,  Jie Yang  1 ,  Yuhang Miao  1 ,  Xiaojing Wang  2 ,  Jie Sun  3
Affiliations
  • 1. School 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.
  • 2. School 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. Electronic address: [email protected].
  • 3. School 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. Electronic address: [email protected].
PMID: 31882295 DOI: 10.1016/j.bmcl.2019.126900
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.

Keywords
4-Arylcoumarins; Alzheimer's disease; Antioxidant activity; Cholinesterase inhibitors; Monoamine oxidase.
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