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Bis-huperzine B: Highly Potent and Selective Acetylcholinesterase Inhibitors

2005; American Chemical Society; Volume: 48; Issue: 3 Linguagem: Inglês

10.1021/jm0496178

1520-4804

Song Feng, Zhifei Wang, Xuchang He, Suxin Zheng, Yu Xia, Hualiang Jiang, Xi-Can Tang, Donglu Bai,

Computational Drug Discovery Methods

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.