Synthesis and bioactivity of novel C2-glycosyl triazole derivatives as acetylcholinesterase inhibitors

Author:

Yin Long1,Wang Lei1,Liu Xiu-Jian1,Cheng Feng-Chang2,Shi Da-Hua13,Cao Zhi-Ling13,Liu Wei-Wei134

Affiliation:

1. College of Pharmaceutical Sciences, Huaihai Institute of Technology, Lianyungang 222005, P.R. China

2. China University of Mining and Technology, Xuzhou 221116, P.R. China

3. Jiangsu Institute of Marine Resources, Lianyungang 222005, P.R. China

4. Jiangsu Key Laboratory of Marine Pharmaceutical Compound Screening, Huaihai Institute of Technology, Lianyungang 222005, P.R. China

Abstract

AbstractNew C2-glycosyl triazole derivatives 6a–l were synthesized by cyclization of glycosyl acylthiosemicarbazides 5 in refluxing 3 N sodium hydroxide aqueous solution. Substrates 5 were obtained by the reaction of glycosyl isothiocyanate 3 with various hydrazides. The acetylcholinesterase (AChE) inhibitory activities of compounds 6 were tested by Ellman’s method. Compounds that exhibited over 85% inhibition were subsequently evaluated for the IC50 values. Compound 6f possesses the best acetylcholinesterase-inhibition activity with IC50 of 1.46±0.25 μg/mL.

Publisher

Walter de Gruyter GmbH

Subject

Organic Chemistry

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