Citation: FENG Jian-An, JIANG Xue-Hua. Synthesis and Evaluation of Two Novel Naphthol Derivatives as Novel Cholinesterase Inhibitors[J]. Chinese Journal of Structural Chemistry, ;2016, 35(3): 371-374. doi: 10.14102/j.cnki.0254-5861.2011-0881 shu

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

FENG Jian-An ,
JIANG Xue-Hua ^,

1.
West China School of Pharmacy, Sichuan University, Chengdu 610041, China

Corresponding author: JIANG Xue-Hua,
Received Date: 3 July 2015
Available Online: 1 December 2015

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) Å, β = 94.716(5)°, V = 3316.9(3) Å³, Z = 8, F(000) = 1384, D_c = 1.511 Mg/m³, M_r = 377.22 and μ = 2.487 mm^-1. In addition, their cholinesterase inhibitory activities in vitro toward Electrophorus electricus acetylcholinesterase (eelAChE) and horse serum butyrylcholinesterase (eqBChE) were further determined. The results showed that compound 1 as a new acetylcholinesterase (AChE) inhibitor displayed higher AChE inhibitory activity (IC₅₀ = 1.4 μM), which could be considered for Alzheimer’s disease therapeutics.
- naphthol,
- crystal,
- cholinesterase
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