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| 引用本文： | �¿���,������,���Ʒ�,���,��ӱ��,���,�����. ����L-����������������ơ��ϳɼ��������������ø�����ƻ����о�[J]. 中国药学杂志, 2015, 50(14): 1180-1185. DOI: 10.11669/cpj.2015.14.004 |
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| 作者姓名： | �¿��� ������ ���Ʒ� ��� ��ӱ�� ��� ����� |
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| 作者单位： | 1. ?????????,???????????????????????????, ??? ???? 071002;
2. ???????????????????,??? ???? 072655 |
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| 摘 要： |
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| 关 键 词： | L-???????? ???????????????? ??????????? |
Design,Synthesis and Evaluation of New L-Phenylalanine Derivatives as Acetylcholinesterase Inhibitors |
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| CHEN Jun-tao,CAO Ting-ting,TIAN Yun-feng,LI Jun-jie,ZHANG Ying-chao,XU Feng,MA Zheng-yue. Design,Synthesis and Evaluation of New L-Phenylalanine Derivatives as Acetylcholinesterase Inhibitors[J]. Chinese Pharmaceutical Journal, 2015, 50(14): 1180-1185. DOI: 10.11669/cpj.2015.14.004 |
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| Authors: | CHEN Jun-tao CAO Ting-ting TIAN Yun-feng LI Jun-jie ZHANG Ying-chao XU Feng MA Zheng-yue |
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| Affiliation: | 1.Key Laboratory of Drug Quality Control of Hebei Province, College of Pharmaceutical Sciences, Hebei University, Baoding 071002, China;2. Hebei Zhitong Biological Pharmaceutical Industry Co., Ltd, Baoding 072655, China |
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| Abstract: | ??OBJECTIVE To research the effect of new L-phenylalanine derivatives on acetylcholinesterase(AChE) activity. METHODS New L-phenylalanine derivatives were synthesized from substituted 2-bromo-1-acetophenones by four steps reaction, and their inhibitory activities on AChE were measured by Ellman method in vitro. RESULTS The evaluation results showed that most derivatives possessed AChE inhibitory effect and the activity of compound 8b was the most potent with an IC50 value of 8.73??10-6 mol??L-1, which was more potent than that of rivastigmine; moreover, compound 8b had no inhibitory activities to BuChE. CONCLUSION The inhibitory activities of new L-phenylalanine derivatives on acetylcholinesterase are worth studying further.
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