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
文献类型：期刊论文
| 作者 | Xu He Nan3; Jin Zhe2; Liu Si Jie2; Liu Hong Min3; Li Shuo1; Lin Huang Quan1; Wan David Chicheong1; Hu Chun3 |
| 刊名 | CHINESE CHEMICAL LETTERS
 |
| 出版日期 | 2012 |
| 卷号 | 23期号:7页码:765-768 |
| 关键词 | ALZHEIMERS-DISEASE Acetylcholinesterase inhibitor Bromination Heterocycle Synthesis 7H-Thiazolo3,2-b-1, 2, 4-triazin-7-one derivatives |
| ISSN号 | 1001-8417 |
| 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 |
| 英文摘要 | 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. |
| 资助项目 | [National Natural Science Foundation of China] |
| 语种 | 英语 |
| CSCD记录号 | CSCD:4595729 |
| 源URL | [http://ir.imr.ac.cn/handle/321006/156053]  |
| 专题 | 金属研究所_中国科学院金属研究所 |
| 作者单位 | 1.中国科学院地质与地球物理研究所 2.中国科学院金属研究所 3.郑州大学 |
| 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. |
入库方式： OAI收割
来源：金属研究所
浏览0
下载0
收藏0
其他版本
除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。