Design, Synthesis, and Evaluation of Chalcone Derivatives as Multifunctional Agents against Alzheimer's Disease

• Published in: Chemistry & biodiversity Vol. 18; no. 11; pp. e2100341 - n/a
• Main Authors: Wang, Xiao‐Qin, Zhou, Lu‐Yi, Tan, Ren‐Xian, Liang, Guo‐Peng, Fang, Si‐Xian, Li, Wei, Xie, Mei, Wen, Yu‐Hao, Wu, Jia‐Qiang, Chen, Yi‐Ping
• Format: Journal Article
• Language: English
• Published: Switzerland Wiley Subscription Services, Inc 01.11.2021
• Subjects: Agglomeration; Alzheimer Disease - drug therapy; Alzheimer Disease - metabolism; Alzheimer's disease; Amyloid beta-Peptides - antagonists & inhibitors; Amyloid beta-Peptides - metabolism; Animals; Antioxidants; Aβ aggregation; Cell Survival - drug effects; chalcone; Chalcones - chemical synthesis; Chalcones - chemistry; Chalcones - pharmacology; Chelation; Copper; Copper - pharmacology; Cytotoxicity; Drug Design; Fibrils; Humans; Memory Disorders - chemically induced; Memory Disorders - drug therapy; metal chelating; Mice; multifunctional; Neurodegenerative diseases; Neuroprotective Agents - chemical synthesis; Neuroprotective Agents - chemistry; Neuroprotective Agents - pharmacology; Peptide Fragments - antagonists & inhibitors; Peptide Fragments - metabolism; Protein Aggregates - drug effects; Scopolamine; Toxicity; Tumor Cells, Cultured; chalcone; Aβ aggregation; multifunctional; Alzheimer's disease; metal chelating

Fifteen chalcone derivatives 3a–3o were synthesized, and evaluated as multifunctional agents against Alzheimer's disease. In vitro studies revealed that these compounds inhibited self‐induced Aβ1‐42 aggregation effectively ranged from 45.9–94.5 % at 20 μM, and acted as potential antioxidants. T...