| Synthesis and biological activity of 3,6-diaryl-7H-thiazolo3,2-b 1,2,4triazin-7-one derivatives as novel acetylcholinesterase inhibitors | |
| Alternative Title | Synthesis and biological activity of 3,6-diaryl-7H-thiazolo3,2-b1,2,4triazin-7-one derivatives as novel acetylcholinesterase inhibitors |
| Jin Zhe1; Yang Liu1; Xu HeNan1; Huang ErFang1; Wan David ChiCheong2; Li Shuo2; Lin HuangQuan2; Hu Chun1 | |
| 2010 | |
| Source Publication | SCIENCE CHINA-CHEMISTRY
 |
| ISSN | 1674-7291 |
| Volume | 53Issue:11Pages:2297-2303 |
| Abstract | 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. |
| Other Abstract | 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 |
| Keyword | AMYLOID-BETA ENZYME DESIGN acetylcholinesterase inhibitor thiazole 1,2,4-triazine heterocycle synthesis docking MVD |
| Indexed By | CSCD |
| Language | 英语 |
| Funding Project | [National Natural Science Foundation of China (NSFC)] |
| CSCD ID | CSCD:4109320 |
| Citation statistics | |
| Document Type | 期刊论文 |
| Identifier | http://ir.imr.ac.cn/handle/321006/158045 |
| Collection | 中国科学院金属研究所 |
| Affiliation | 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 |
| Recommended Citation 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. |
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