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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
Alternative TitleDesign, 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 Nan1; Jin Zhe2; Liu Si Jie2; Liu Hong Min1; Li Shuo3; Lin Huang Quan3; Wan David Chicheong3; Hu Chun1
2012
Source PublicationCHINESE CHEMICAL LETTERS
ISSN1001-8417
Volume23Issue:7Pages:765-768
AbstractBromination 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.
Other AbstractBromination 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.
KeywordALZHEIMERS-DISEASE Acetylcholinesterase inhibitor Bromination Heterocycle Synthesis 7H-Thiazolo3,2-b-1, 2, 4-triazin-7-one derivatives
Indexed ByCSCD
Language英语
Funding Project[National Natural Science Foundation of China]
CSCD IDCSCD:4595729
Citation statistics
Document Type期刊论文
Identifierhttp://ir.imr.ac.cn/handle/321006/156054
Collection中国科学院金属研究所
Affiliation1.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
Recommended Citation
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.
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