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他克林-E2020杂合物作为治疗阿尔茨海默病的乙酰胆碱酯酶抑制剂的合成与评价

Synthesis and evaluation of tacrine-E2020 hybrids as acetylcholinesterase inhibitors for the treatment of Alzheimer's disease.

作者信息

Shao Dong, Zou Chunyan, Luo Cheng, Tang Xican, Li Yuanchao

机构信息

Shanghai Institute of Materia Medica, Shanghai Institute for Biological Sciences, Graduate School of the Chinese Academy of Sciences, 555 Zhu Chong Zhi Road, Zhangjiang Hi-Tech Park, Shanghai 201203, China.

出版信息

Bioorg Med Chem Lett. 2004 Sep 20;14(18):4639-42. doi: 10.1016/j.bmcl.2004.07.005.

DOI:10.1016/j.bmcl.2004.07.005
PMID:15324879
Abstract

Tacrine-E2020 hybrids and some related compounds were prepared and their bioactivities on the Alzheimer's disease were assayed. The optimum hybrid inhibitor 3 is 37-fold more potent and 31-fold more selective than tacrine in vitro.

摘要

制备了他克林-E2020杂合物及一些相关化合物，并测定了它们对阿尔茨海默病的生物活性。最佳杂合抑制剂3在体外的效力比他克林高37倍，选择性高31倍。

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