| Design, Synthesis, and Biological Evaluation of 5H-Thiazolo3,2-apyrimidine-6-carboxylic Acid Ethyl Ester Derivatives as a Novel Series of Acetylcholinesterase Inhibitors | |
| Alternative Title | Design, Synthesis, and Biological Evaluation of 5H-Thiazolo3,2-apyrimidine-6-carboxylic Acid Ethyl Ester Derivatives as a Novel Series of Acetylcholinesterase Inhibitors |
| Zhi Hui1; Chen Lanmei1; Zhang Linlin1; Liu Sijie1; Wan David Chi Cheong2; Lin Huangquan2; Hu Chun1 | |
| 2009 | |
| Source Publication | CHEMICAL RESEARCH IN CHINESE UNIVERSITIES
 |
| ISSN | 1005-9040 |
| Volume | 25Issue:3Pages:332-337 |
| Abstract | Acetylcholinesterase inhibitors are the most frequently prescribed anti-Alzheimer's drugs. A series of 5H-thiazolo3,2-apyrimidine-6-carboxylic acid ethyl ester derivatives as the novel acetylcholinesterase inhibitors was designed based on virtual screening methods. The target compounds were synthesized with Biginelli reaction and Hantzsch-type condensation of dihydropyrimidines with substituted phenacyl chlorides, and were characterized with elemental analysis, IR, MS, H-1 NMR, and C-13 NMR. The biological evaluation against human acetylcholinesterase in vitro indicated all the target compounds show more than 50% inhibition at 10 mu mol/L by means of the Ellman method. The results provide a starting point for the development of novel drugs to treat Alzheimer's disease and lay the foundation of searching for improved acetylcholinesterase inhibitors with the novel scaffolds. |
| Other Abstract | Acetylcholinesterase inhibitors are the most frequently prescribed anti-Alzheimer's drugs. A series of 5H-thiazolo3,2-apyrimidine-6-carboxylic acid ethyl ester derivatives as the novel acetylcholinesterase inhibitors was designed based on virtual screening methods. The target compounds were synthesized with Biginelli reaction and Hantzsch-type condensation of dihydropyrimidines with substituted phenacyl chlorides, and were characterized with elemental analysis, IR, MS, ~1H NMR, and ~(13)C NMR. The biological evaluation against human acetylcholinesterase in vitro indicated all the target compounds show more than 50% inhibition at 10 μmol/L by means of the Ellman method. The results provide a starting point for the development of novel drugs to treat Alzheimer's disease and lay the foundation of searching for improved acetylcholinesterase inhibitors with the novel scaffolds. |
| Keyword | Acetylcholinesterase inhibitor Docking screening Heterocycle Biological activity 5H-Thiazolo3,2-a pyrimidine-6-carboxylic acid ethyl ester derivative |
| Indexed By | CSCD |
| Language | 英语 |
| CSCD ID | CSCD:3684013 |
| Citation statistics |
Cited Times:1[CSCD]
[CSCD Record]
|
| Document Type | 期刊论文 |
| Identifier | http://ir.imr.ac.cn/handle/321006/144615 |
| 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 | Zhi Hui,Chen Lanmei,Zhang Linlin,et al. Design, Synthesis, and Biological Evaluation of 5H-Thiazolo3,2-apyrimidine-6-carboxylic Acid Ethyl Ester Derivatives as a Novel Series of Acetylcholinesterase Inhibitors[J]. CHEMICAL RESEARCH IN CHINESE UNIVERSITIES,2009,25(3):332-337. |
| APA | Zhi Hui.,Chen Lanmei.,Zhang Linlin.,Liu Sijie.,Wan David Chi Cheong.,...&Hu Chun.(2009).Design, Synthesis, and Biological Evaluation of 5H-Thiazolo3,2-apyrimidine-6-carboxylic Acid Ethyl Ester Derivatives as a Novel Series of Acetylcholinesterase Inhibitors.CHEMICAL RESEARCH IN CHINESE UNIVERSITIES,25(3),332-337. |
| MLA | Zhi Hui,et al."Design, Synthesis, and Biological Evaluation of 5H-Thiazolo3,2-apyrimidine-6-carboxylic Acid Ethyl Ester Derivatives as a Novel Series of Acetylcholinesterase Inhibitors".CHEMICAL RESEARCH IN CHINESE UNIVERSITIES 25.3(2009):332-337. |
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