Potent, easily synthesized huperzine A-tacrine hybrid acetylcholinesterase inhibitors

被引：79

作者：

Carlier, PR ^{[1
]}

Du, DM

Han, YF

Liu, J

Pang, YP

机构：

[1] Hong Kong Univ Sci & Technol, Dept Chem, Clear Water Bay, Kowloon, Peoples R China

[2] Hong Kong Univ Sci & Technol, Dept Biochem, Kowloon, Peoples R China

[3] Mayo Clin, Dept Pharmacol, Mayo Canc Ctr, Rochester, MN 55905 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 16期

关键词：

D O I：

10.1016/S0960-894X(99)00396-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Hybrid acetylcholinesterase inhibitors composed of a key fragment of huperzine A and an intact tacrine unit were prepared. The syntheses are quite direct, proceeding in a maximum of 4 linear steps from commercially available starting materials. The optimum hybrid inhibitor (+/-)-9g is 13-fold more potent than (-)-huperzine A, and 25-fold more potent than tacrine. (C) 1999 Elsevier Science Ltd. All rights reserved.

引用

页码：2335 / 2338

页数：4

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