Synthesis and biological evaluation of helicid analogues as novel acetylcholinesterase inhibitors

[摘要]：

A series of helicid analogues were prepared and evaluated in vitro for the cholinesterase (AChE and BuChE) inhibitory activities via UV spectroscopy. The results indicated that compounds 5, 6d and 8 exhibited potent AChE inhibitory activities with IC50 values of 0.45 +/- 0.02 mu M 0.49 +/- 0.02 mu M, and 0.20 +/- 0.01 mu M, respectively. High selectivity for AChE over BuChE was also observed. Kinetic study showed that the mechanism of AChE inhibition of compounds 5, 6d and 8 was all mixed-type. (C) 2007 Elsevier Masson SAS. All rights reserved.

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