Synthesis and Evaluation of Two Novel Naphthol Derivatives as Novel Cholinesterase Inhibitors  

作　　者：冯建安 蒋学华 

机构地区：[1]West China School of Pharmacy,Sichuan University

出　　处：《Chinese Journal of Structural Chemistry》2016年第3期371-374,共4页结构化学（英文）

摘　　要：Two novel naphthol derivatives（1 and 2） were synthesized and characterized via IR,~1H NMR,and HRMS.The structure of compound 2 was verified by single-crystal X-ray crystallography.It crystallizes in monoclinic,space group C2/c with a = 21.6725（9）,b = 6.0127（3）,c = 25.5405（14） A,β = 94.716（5）o,V = 3316.9（3） A^3,Z = 8,F（000） = 1384,D_c = 1.511 Mg/m^3,M_r = 377.22 and μ = 2.487 mm^-1.In addition,their cholinesterase inhibitory activities in vitro toward Electrophorus electricus acetylcholinesterase（eel ACh E） and horse serum butyrylcholinesterase（eq BCh E） were further determined.The results showed that compound 1 as a new acetylcholinesterase（ACh E） inhibitor displayed higher ACh E inhibitory activity（IC_（50） = 1.4 μM）,which could be considered for Alzheimer＇s disease therapeutics.Two novel naphthol derivatives（1 and 2） were synthesized and characterized via IR,~1H NMR,and HRMS.The structure of compound 2 was verified by single-crystal X-ray crystallography.It crystallizes in monoclinic,space group C2/c with a = 21.6725（9）,b = 6.0127（3）,c = 25.5405（14） A,β = 94.716（5）o,V = 3316.9（3） A^3,Z = 8,F（000） = 1384,D_c = 1.511 Mg/m^3,M_r = 377.22 and μ = 2.487 mm^-1.In addition,their cholinesterase inhibitory activities in vitro toward Electrophorus electricus acetylcholinesterase（eel ACh E） and horse serum butyrylcholinesterase（eq BCh E） were further determined.The results showed that compound 1 as a new acetylcholinesterase（ACh E） inhibitor displayed higher ACh E inhibitory activity（IC_（50） = 1.4 μM）,which could be considered for Alzheimer＇s disease therapeutics.

关 键 词：naphthol crystal cholinesterase 

分 类 号：O625.313[理学—有机化学] TQ460.1[理学—化学]