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Design, Synthesis, and Biological Evaluation of 5H-Thiazolo3,2-apyrimidine-6-carboxylic Acid Ethyl Ester Derivatives as a Novel Series of Acetylcholinesterase Inhibitors
Alternative TitleDesign, 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 PublicationCHEMICAL RESEARCH IN CHINESE UNIVERSITIES
ISSN1005-9040
Volume25Issue:3Pages:332-337
AbstractAcetylcholinesterase 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 AbstractAcetylcholinesterase 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.
KeywordAcetylcholinesterase inhibitor Docking screening Heterocycle Biological activity 5H-Thiazolo3,2-a pyrimidine-6-carboxylic acid ethyl ester derivative
Indexed ByCSCD
Language英语
CSCD IDCSCD:3684013
Citation statistics
Document Type期刊论文
Identifierhttp://ir.imr.ac.cn/handle/321006/144613
Collection中国科学院金属研究所
Affiliation1.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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