Design, synthesis characterization and in vitro biological activity of a series of 3-aryl-6-(bromoarylmethyl)-7H-thiazolo3,2-b-1, 2, 4-triazin-7-one derivatives as the novel acetylcholinesterase inhibitors

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	Design, synthesis characterization and in vitro biological activity of a series of 3-aryl-6-(bromoarylmethyl)-7H-thiazolo3,2-b-1, 2, 4-triazin-7-one derivatives as the novel acetylcholinesterase inhibitors
其他题名	Design, synthesis characterization and in vitro biological activity of a series of 3-aryl-6-(bromoarylmethyl)-7H-thiazolo3,2-b-1, 2, 4-triazin-7-one derivatives as the novel acetylcholinesterase inhibitors
	Xu He Nan 1; Jin Zhe 2; Liu Si Jie 2; Liu Hong Min 1; Li Shuo 3; Lin Huang Quan 3; Wan David Chicheong 3; Hu Chun 1
	2012
发表期刊	CHINESE CHEMICAL LETTERS
ISSN	1001-8417
卷号	23 期号:7 页码:765-768
摘要	Bromination is used as a strategy to improve biological activity in medicinal chemistry. In order to study on the structure activity relationships of the novel acetylcholinesterase inhibitors with 7H-thiazolo3,2-b-1, 2, 4-triazin-7-one scaffold, based on our previous work and molecular modeling, a series of novel 3-aryl-6-(bromoarylmethyl)-7H-thiazolo3,2-b-1, 2, 4-triazin-7-one derivatives were designed by molecular docking, synthesized and characterized by mass spectra, infrared spectra, proton NMR and elemental analyses. The study of AChE inhibitory activity was carried out using the Ellman colorimetric assay with huperzine-A as the positive control. Most of all target compounds exhibited more than 45% inhibition at 10 mu mol/L. The preliminary structure-activity relationship was the bromine atoms and the hydroxyl group at the phenyl ring at the C6 position of the parent nucleus played significant roles in the AChE inhibitory activity of the target compounds. (c) 2012 Hong Min Liu. Published by Elsevier B.V. on behalf of Chinese Chemical Society. All rights reserved.
其他摘要	Bromination is used as a strategy to improve biological activity in medicinal chemistry.In order to study on the structure-activity relationships of the novel acetylcholinesterase inhibitors with 7H-thiazolo3,2-b-1,2,4-triazin-7-one scaffold,based on our previous work and molecular modeling,a series of novel 3-aryl-6-(bromoarylrnethyl)-7H-thiazolo3,2-b-1,2,4-triazin-7-one derivatives were designed by molecular docking,synthesized and characterized by mass spectra,infrared spectra,proton NMR and elemental analyses.The study of AChE inhibitory activity was carried out using the Ellman colorimetric assay with huperzine-A as the positive control.Most of all target compounds exhibited more than 45%inhibition at 10μmol/L.The preliminary structureactivity relationship was the bromine atoms and the hydroxyl group at the phenyl ring at the C6 position of the parent nucleus played significant roles in the AChE inhibitory activity of the target compounds.
关键词	ALZHEIMERS-DISEASE Acetylcholinesterase inhibitor Bromination Heterocycle Synthesis 7H-Thiazolo3,2-b-1, 2, 4-triazin-7-one derivatives
收录类别	CSCD
语种	英语
资助项目	[National Natural Science Foundation of China]
CSCD记录号	CSCD:4595729
引用统计
文献类型	期刊论文
条目标识符	http://ir.imr.ac.cn/handle/321006/156054
专题	中国科学院金属研究所
作者单位	1.郑州大学 2.中国科学院金属研究所 3.中国科学院地质与地球物理研究所
推荐引用方式 GB/T 7714	Xu He Nan,Jin Zhe,Liu Si Jie,et al. Design, synthesis characterization and in vitro biological activity of a series of 3-aryl-6-(bromoarylmethyl)-7H-thiazolo3,2-b-1, 2, 4-triazin-7-one derivatives as the novel acetylcholinesterase inhibitors[J]. CHINESE CHEMICAL LETTERS,2012,23(7):765-768.
APA	Xu He Nan.,Jin Zhe.,Liu Si Jie.,Liu Hong Min.,Li Shuo.,...&Hu Chun.(2012).Design, synthesis characterization and in vitro biological activity of a series of 3-aryl-6-(bromoarylmethyl)-7H-thiazolo3,2-b-1, 2, 4-triazin-7-one derivatives as the novel acetylcholinesterase inhibitors.CHINESE CHEMICAL LETTERS,23(7),765-768.
MLA	Xu He Nan,et al."Design, synthesis characterization and in vitro biological activity of a series of 3-aryl-6-(bromoarylmethyl)-7H-thiazolo3,2-b-1, 2, 4-triazin-7-one derivatives as the novel acetylcholinesterase inhibitors".CHINESE CHEMICAL LETTERS 23.7(2012):765-768.