Design, Synthesis, and Biological Evaluation of 5H-Thiazolo3,2-apyrimidine-6-carboxylic Acid Ethyl Ester Derivatives as a Novel Series of Acetylcholinesterase Inhibitors

IMR OpenIR

	Design, Synthesis, and Biological Evaluation of 5H-Thiazolo3,2-apyrimidine-6-carboxylic Acid Ethyl Ester Derivatives as a Novel Series of Acetylcholinesterase Inhibitors
其他题名	Design, Synthesis, and Biological Evaluation of 5H-Thiazolo3,2-apyrimidine-6-carboxylic Acid Ethyl Ester Derivatives as a Novel Series of Acetylcholinesterase Inhibitors
	Zhi Hui 1; Chen Lanmei 1; Zhang Linlin 1; Liu Sijie 1; Wan David Chi Cheong 2; Lin Huangquan 2; Hu Chun 1
	2009
发表期刊	CHEMICAL RESEARCH IN CHINESE UNIVERSITIES
ISSN	1005-9040
卷号	25 期号:3 页码:332-337
摘要	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.
其他摘要	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.
关键词	Acetylcholinesterase inhibitor Docking screening Heterocycle Biological activity 5H-Thiazolo3,2-a pyrimidine-6-carboxylic acid ethyl ester derivative
收录类别	CSCD
语种	英语
CSCD记录号	CSCD:3684013
引用统计	被引频次：1[CSCD] [CSCD记录]
文献类型	期刊论文
条目标识符	http://ir.imr.ac.cn/handle/321006/144613
专题	中国科学院金属研究所
作者单位	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
推荐引用方式 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.