Synthesis of derivatives of cleistopholine and their anti-acetylcholinesterase and anti-β-amyloid aggregation activity

A series of 6- and 9-substituted cleistopholine derivatives have been synthesized and tested for their ability to inhibit cholinesterase and β-amyloid aggregation in vitro. Their blood-brain barrier permeability was also assessed. [Display omitted] •The new cleistopholine derivatives exhibited high...

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Veröffentlicht in:	Bioorganic chemistry 2018-02, Vol.76, p.228-236
Hauptverfasser:	Wu, Zhenhua, Liao, Wenxia, Chen, Kelin, Qin, Jingfang, Tang, Huang
Format:	Artikel
Sprache:	eng
Schlagworte:	Acetylcholinesterase - metabolism Amyloid beta-Peptides - antagonists & inhibitors Amyloid beta-Peptides - metabolism Animals Anthraquinones - chemical synthesis Anthraquinones - pharmacology Aza Compounds - chemical synthesis Aza Compounds - pharmacology Blood-Brain Barrier - drug effects Butyrylcholinesterase - metabolism Cell Line, Tumor Cholinesterase inhibitor Cholinesterase Inhibitors - chemical synthesis Cholinesterase Inhibitors - pharmacology Cleistopholine derivative Electrophorus Enzyme Assays Horses Humans Peptide Fragments - antagonists & inhibitors Peptide Fragments - metabolism Permeability - drug effects Synthesis β-Amyloid aggregation
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