Design, synthesis, and biological evaluation of novel indanone-based hybrids as multifunctional cholinesterase inhibitors for Alzheimer's disease

Journal of Molecular Structure(2021)

引用 12|浏览3
暂无评分
摘要
•Novel indanone-carbamate (inspired from donepezil-rivastigmine) with anti-ChE activity were designed and synthesized.•X-ray structure analysis for the chiral center of 4a was assigned.•In vitro anti-ChE activities of the novel compounds were determined and AChE and BChE inhibition mechanisms of the most potent derivative were studied.•Interactions of derivative with predicted allosteric binding site (based on the result of the kinetic study) on AChE and BChE were studied using docking studies.•Good neuroprotective and anti-Aβ aggregation activities were shown for the potent compounds.
更多
查看译文
关键词
Acetylcholinesterase inhibitor,Alzheimer's disease,Amyloid-β self-aggregation,crystallography analysis,Indanone-carbamate hybrid,Structure-activity relationship,Molecular docking,Neuroprotection,Partial non-competitive mixed-type inhibition
AI 理解论文
溯源树
样例
生成溯源树,研究论文发展脉络
Chat Paper
正在生成论文摘要