- Synthesis and biological evaluation of helicid analogues as novel acetylcholinesterase inhibitors.
Synthesis and biological evaluation of helicid analogues as novel acetylcholinesterase inhibitors.
European journal of medicinal chemistry (2007-06-19)
Huan Wen, Chonglan Lin, Ling Que, Hui Ge, Lin Ma, Rihui Cao, Yiqian Wan, Wenlie Peng, Zihou Wang, Huacan Song
PMID17574306
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 IC(50) values of 0.45+/-0.02microM, 0.49+/-0.02microM, and 0.20+/-0.01microM, 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.