Synthesis and biological evaluation of 4-arylcoumarins as potential anti-Alzheimer's disease agents
| Autor: | Yuhang Miao, Jie Yang, Yinling Yun, Jie Sun, Xiao-Jing Wang |
|---|---|
| Rok vydání: | 2019 |
| Předmět: |
Antioxidant
Monoamine Oxidase Inhibitors Monoamine oxidase medicine.medical_treatment Clinical Biochemistry Pharmaceutical Science Pharmacology 01 natural sciences Biochemistry chemistry.chemical_compound Inhibitory Concentration 50 Structure-Activity Relationship Degenerative disease Alzheimer Disease Coumarins Drug Discovery medicine Humans Molecular Biology Monoamine Oxidase Butyrylcholinesterase Cholinesterase chemistry.chemical_classification Binding Sites biology 010405 organic chemistry Organic Chemistry medicine.disease Acetylcholinesterase In vitro 0104 chemical sciences Protein Structure Tertiary Molecular Docking Simulation 010404 medicinal & biomolecular chemistry Kinetics Enzyme chemistry biology.protein Molecular Medicine Cholinesterase Inhibitors |
| Zdroj: | Bioorganicmedicinal chemistry letters. 30(4) |
| ISSN: | 1464-3405 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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