| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1399881 | European Journal of Medicinal Chemistry | 2008 | 8 Pages |
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.
Graphical abstractA series of helicid analogs 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 inhibitory activities with IC50 value of 0.45 ± 0.02 μM, 0.49 ± 0.02 μM, and 0.20 ± 0.01 μM, respectively. Kinetic study showed that the mechanism of AChE inhibition of compounds 5, 6d and 8 was all mixed-type.Figure optionsDownload full-size imageDownload as PowerPoint slide
