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J Med Chem. 2005 Feb 10;48(3):655-7.

Bis-huperzine B: highly potent and selective acetylcholinesterase inhibitors.

Author information

1
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, 555 Zuchongzhi Road, Zhangjiang, 201203, Shanghai.

Abstract

By targeting dual active sites of AChE, a series of bis-huperzine B analogues with various lengths of the tether were designed, synthesized, and tested for their inhibition and selectivity. The most potent bis-huperzine B (5g) exhibited 3900-fold increase in AChE inhibition and 930-fold greater in selectivity for AChE vs BuChE than its parent huperzine B.

PMID:
15689148
DOI:
10.1021/jm0496178
[Indexed for MEDLINE]

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