Synthesis and biological activity of 3,6-diaryl-7H-thiazolo3,2-b 1,2,4triazin-7-one derivatives as novel acetylcholinesterase inhibitors

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	Synthesis and biological activity of 3,6-diaryl-7H-thiazolo3,2-b 1,2,4triazin-7-one derivatives as novel acetylcholinesterase inhibitors
其他题名	Synthesis and biological activity of 3,6-diaryl-7H-thiazolo3,2-b1,2,4triazin-7-one derivatives as novel acetylcholinesterase inhibitors
	Jin Zhe 1; Yang Liu 1; Xu HeNan 1; Huang ErFang 1; Wan David ChiCheong 2; Li Shuo 2; Lin HuangQuan 2; Hu Chun 1
	2010
发表期刊	SCIENCE CHINA-CHEMISTRY
ISSN	1674-7291
卷号	53 期号:11 页码:2297-2303
摘要	Acetylcholinesterase inhibitors played significant roles in treatment of Alzheimer's disease. Based on the research foundation of our previous work and molecular modeling, twelve 3,6-diaryl-7H-thiazolo3,2-b1,2,4triazin-7-one derivatives were synthesized and characterized by mass spectra, infrared spectra, 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. All target compounds exhibited more than 40% inhibition at 10 mu M. Some target compounds showed good inhibition against AChE. The preliminary structure-activity relationships were the halogen atoms at the phenyl ring at the C6 position, the hydroxy groups and the long side chains at the phenyl ring at the C3 position of the parent nucleus played significant roles in the AChE inhibitory activity of the target compounds.
其他摘要	Acetylcholinesterase inhibitors played significant roles in treatment of Alzheimer's disease. Based on the research foundation of our previous work and molecular modeling, twelve 3,6-diaryl-7H-thiazolo3,2-b1,2,4triazin-7-one derivatives were synthesized and characterized by mass spectra, infrared spectra,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. All target compounds exhibited more than 40%inhibition at 10-M. Some target compounds showed good inhibition against AChE.The preliminary structure-activity relationships were the halogen atoms at the phenyl ring at the C6 position, the hydroxy groups and the long side chains at the phenyl ring at the C3 position of the parent nucleus played significant roles in the AChE inhibitory activity of the target compounds
关键词	AMYLOID-BETA ENZYME DESIGN acetylcholinesterase inhibitor thiazole 1,2,4-triazine heterocycle synthesis docking MVD
收录类别	CSCD
语种	英语
资助项目	[National Natural Science Foundation of China (NSFC)]
CSCD记录号	CSCD:4109320
引用统计
文献类型	期刊论文
条目标识符	http://ir.imr.ac.cn/handle/321006/158045
专题	中国科学院金属研究所
作者单位	1.中国科学院金属研究所 2.中国科学院地质与地球物理研究所
推荐引用方式 GB/T 7714	Jin Zhe,Yang Liu,Xu HeNan,et al. Synthesis and biological activity of 3,6-diaryl-7H-thiazolo3,2-b 1,2,4triazin-7-one derivatives as novel acetylcholinesterase inhibitors[J]. SCIENCE CHINA-CHEMISTRY,2010,53(11):2297-2303.
APA	Jin Zhe.,Yang Liu.,Xu HeNan.,Huang ErFang.,Wan David ChiCheong.,...&Hu Chun.(2010).Synthesis and biological activity of 3,6-diaryl-7H-thiazolo3,2-b 1,2,4triazin-7-one derivatives as novel acetylcholinesterase inhibitors.SCIENCE CHINA-CHEMISTRY,53(11),2297-2303.
MLA	Jin Zhe,et al."Synthesis and biological activity of 3,6-diaryl-7H-thiazolo3,2-b 1,2,4triazin-7-one derivatives as novel acetylcholinesterase inhibitors".SCIENCE CHINA-CHEMISTRY 53.11(2010):2297-2303.