950762-02-4Relevant academic research and scientific papers
Synthesis and biological evaluation of helicid analogues as novel acetylcholinesterase inhibitors
Wen, Huan,Lin, Chonglan,Que, Ling,Ge, Hui,Ma, Lin,Cao, Rihui,Wan, Yiqian,Peng, Wenlie,Wang, Zihou,Song, Huacan
, p. 166 - 173 (2008/09/17)
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 μM, 0.49 ± 0.02 μM, and 0.20 ± 0.01 μM, 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.
