Discovery of novel propargylamine-modified 4-aminoalkyl imidazole substituted pyrimidinylthiourea derivatives as multifunctional agents for the treatment of Alzheimer's disease

A series of novel propargylamine-modified pyrimidinylthiourea derivatives (1–3) were designed and synthesized as multifunctional agents for Alzheimer's disease (AD) therapy, and their potential was evaluated through various biological experiments. Among these derivatives, compound 1b displayed...

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Veröffentlicht in:	European journal of medicinal chemistry 2018-01, Vol.143, p.33-47
Hauptverfasser:	Xu, Yi-xiang, Wang, Huan, Li, Xiao-kang, Dong, Sheng-nan, Liu, Wen-wen, Gong, Qi, Wang, Tian-duan-yi, Tang, Yun, Zhu, Jin, Li, Jian, Zhang, Hai-yan, Mao, Fei
Format:	Artikel
Sprache:	eng
Schlagworte:	Acetylcholinesterase - metabolism AChE inhibitors Alzheimer Disease - drug therapy Alzheimer's disease Animals Butyrylcholinesterase - metabolism Cholinesterase Inhibitors - chemical synthesis Cholinesterase Inhibitors - chemistry Cholinesterase Inhibitors - pharmacology Cognitive Dysfunction - chemically induced Cognitive Dysfunction - drug therapy Dose-Response Relationship, Drug Drug Discovery Humans Imidazoles - chemistry Imidazoles - pharmacology MAO-B inhibitors Metal chelating agents Mice Molecular Structure Monoamine Oxidase - metabolism Monoamine Oxidase Inhibitors - chemical synthesis Monoamine Oxidase Inhibitors - chemistry Monoamine Oxidase Inhibitors - pharmacology Multifunctional agents Pargyline - analogs & derivatives Pargyline - chemistry Pargyline - pharmacology Propylamines - chemistry Propylamines - pharmacology Pyrimidines - chemical synthesis Pyrimidines - chemistry Pyrimidines - pharmacology Rats Scopolamine Hydrobromide Structure-Activity Relationship Thiourea - chemical synthesis Thiourea - chemistry Thiourea - pharmacology
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