Design, synthesis, biological evaluation, and molecular modeling studies of chalcone-rivastigmine hybrids as cholinesterase inhibitors

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• 作者：Ling Wang^a ; ^&dagger ; ; ^{lingwang@scut.edu.cn} ; Yu Wang^b ; ^&dagger ; ; Yiguang Tian^a ; ^&dagger ; ; Jinling Shang^a ; Xiaoou Sun^a ; Hongzhuan Chen^b ; Hao Wang^b ; ^{angela_wanghao@hotmail.com} ; Wen Tan^a ; ^{went@scut.edu.cn}
• 关键词：Cholinesterase inhibition ; Chalcone-rivastigmine hybrids ; Alzheimer&rsquo ; s disease ; Antioxidative ; Molecular docking
• 刊名：Bioorganic & Medicinal Chemistry
• 出版年：2017
• 出版时间：1 January 2017
• 年：2017
• 卷：25
• 期：1
• 页码：360-371
• 全文大小：3471 K
• 卷排序：25

文摘

A series of novel chalcone-rivastigmine hybrids have been designed and synthesized. Biochemical assessment of cholinesterase enzyme has been carried out. Some of the designed compounds showed promising anticholinesterase activity and low toxicity. Compound 3 blocked the formation of reactive oxygen species (ROS) in SH-SY5Y cells. Molecular docking and molecular dynamics simulations studies have been done.