Synthesis, pharmacology and molecular docking on multifunctional tacrine-ferulic acid hybrids as cholinesterase inhibitors against Alzheimer's disease.
作者: Zhu JieYang HongyuChen YaoLin HongzhiLi QiMo JunBian YaoyaoPei YuqiongSun Haopeng
作者单位: 1a Department of Medicinal Chemistry , China Pharmaceutical University , Nanjing , China.
2b School of Pharmacy , Nanjing University of Chinese Medicine , Nanjing , China.
3c School of Nursing , Nanjing University of Chinese Medicine , Nanjing , China.
刊名: Journal of enzyme inhibition and medicinal chemistry, 2018, Vol.33 (1), pp.496-506
来源数据库: PubMed Journal
DOI: 10.1080/14756366.2018.1430691
关键词: Alzheimer’s diseaseCholinesterase inhibitorMolecular dockingMulti-target ligandTacrine-ferulic hybrid
原始语种摘要: The cholinergic hypothesis has long been a "polar star" in drug discovery for Alzheimer's disease (AD), resulting in many small molecules and biological drug candidates. Most of the drugs marketed for AD are cholinergic. Herein, we report our efforts in the discovery of cholinesterases inhibitors (ChEIs) as multi-target-directed ligands. A series of tacrine-ferulic acid hybrids have been designed and synthesised. All these compounds showed potent acetyl-(AChE) and butyryl cholinesterase(BuChE) inhibition. Among them, the optimal compound 10g, was the most potent inhibitor against AChE (electrophorus electricus (eeAChE) half maximal inhibitory concentration (IC50) = 37.02 nM), it was also a strong inhibitor against BuChE (equine serum (eqBuChE) IC50 = 101.40 nM)....
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关键词翻译
关键词翻译
  • tacrine 他克林
  • cholinesterase 胆碱酯酶
  • against 反对
  • pharmacology 药理学
  • cholinergic 胆碱能的
  • disease 
  • docking 靠泊
  • impairment 减损
  • potent 强大的
  • electrophorus 起电盘