Design, Synthesis and Evaluation of Novel Tacrine-Ferulic Acid Hybrids as Multifunctional Drug Candidates against Alzheimer’s Disease

Autor: Hui Lei, Yingbo Fu, Zhanyou Wang, Xiaodan Qu, Li Han, Pu Wang, Qiao Leng, Yu Mu, Xueshi Huang, Xin Li
Jazyk: angličtina
Rok vydání: 2016
Předmět:
0301 basic medicine
β-amyloid aggregation
cholinesterase
ferulic acid
metal chelator
tacrine
neuroprotection
Pharmaceutical Science
01 natural sciences
Analytical Chemistry
Ferulic acid
chemistry.chemical_compound
Drug Discovery
Chelating Agents
biology
Molecular Structure
Chemistry
Molecular Docking Simulation
Biochemistry
Chemistry (miscellaneous)
Tacrine
language
Acetylcholinesterase
Molecular Medicine
medicine.drug
Coumaric Acids
Aché
Cell Survival
Neuroprotection
Article
Cell Line
lcsh:QD241-441
03 medical and health sciences
Structure-Activity Relationship
lcsh:Organic chemistry
Alzheimer Disease
medicine
Humans
Chelation
Physical and Theoretical Chemistry
Cholinesterase
Amyloid beta-Peptides
010405 organic chemistry
Organic Chemistry
Neurotoxicity
medicine.disease
language.human_language
In vitro
0104 chemical sciences
030104 developmental biology
Butyrylcholinesterase
Drug Design
biology.protein
Cholinesterase Inhibitors
Zdroj: Molecules, Vol 21, Iss 10, p 1338 (2016)
Scopus-Elsevier
Molecules; Volume 21; Issue 10; Pages: 1338
Molecules
ISSN: 1420-3049
Popis: Five novel tacrine-ferulic acid hybrid compounds (8a–e) were synthesized and their structures were identified on the basis of a detailed spectroscopic analysis. The activities of inhibiting acetyl cholinesterase (AChE) and butyryl cholinesterase (BuChE), reducing self-induced β-amyloid (Aβ) aggregation and chelating Cu2+ were evaluated in vitro. Among them, 8c and 8d displayed the higher selectivity in inhibiting AChE over BuChE. Moreover, 8d also showed dramatic inhibition of self-Aβ aggregation, activity of chelating Cu2+ and activity against Aβ-induced neurotoxicity in Neuro-2A cells.
Databáze: OpenAIRE
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