Abstract
The docking study on a series of 7H-thiazolo[3,2-b]-1,2,4-triazin-7-one derivatives with acetylcholinesterase has been demonstrated. The synthesis and characterization of a series of 7H-thiazolo[3,2-b]-1,2,4-triazin-7-one derivatives were described. All target compounds were evaluated in vitro for the inhibitory activities against AChE via Ellman colorimetric assay. Most of the target compounds possessed anti-acetylcholinesterase activity. The preliminary structure-activity relationships were discussed.
Keywords: Acetylcholinesterase, Inhibitors, Synthesis, Heterocycles, Docking, 7H-thiazolo[3,2-b]-1,2,4-triazin-7-one derivative
Letters in Drug Design & Discovery
Title: Design, Synthesis, and Biological Evaluation of 7H-thiazolo[3,2-b]-1,2,4-triazin-7-one Derivatives as Acetylcholinesterase Inhibitors
Volume: 7 Issue: 1
Author(s): Si-Jie Liu, Liu Yang, Xiao-Guang Liu, Ying Luo, Zi-Jian Cao, David Chi Cheong Wan, Huang-Quan Lin and Chun Hu
Affiliation:
Keywords: Acetylcholinesterase, Inhibitors, Synthesis, Heterocycles, Docking, 7H-thiazolo[3,2-b]-1,2,4-triazin-7-one derivative
Abstract: The docking study on a series of 7H-thiazolo[3,2-b]-1,2,4-triazin-7-one derivatives with acetylcholinesterase has been demonstrated. The synthesis and characterization of a series of 7H-thiazolo[3,2-b]-1,2,4-triazin-7-one derivatives were described. All target compounds were evaluated in vitro for the inhibitory activities against AChE via Ellman colorimetric assay. Most of the target compounds possessed anti-acetylcholinesterase activity. The preliminary structure-activity relationships were discussed.
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Liu Si-Jie, Yang Liu, Liu Xiao-Guang, Luo Ying, Cao Zi-Jian, Cheong Wan Chi David, Lin Huang-Quan and Hu Chun, Design, Synthesis, and Biological Evaluation of 7H-thiazolo[3,2-b]-1,2,4-triazin-7-one Derivatives as Acetylcholinesterase Inhibitors, Letters in Drug Design & Discovery 2010; 7 (1) . https://dx.doi.org/10.2174/157018010789869343
DOI https://dx.doi.org/10.2174/157018010789869343 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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