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Table 1 Inhibitory effect of compounds 1–10 on human AChE and BChE

From: Synthesis and biological evaluation of lycorine derivatives as dual inhibitors of humanacetylcholinesterase and butyrylcholinesterase

Lycorine analogue

No.

IC50(μM)

 

hAChE

hBChE

1,2-O,O'-Dibenzoyllycorine

1

> 50

7.72 ± 0.26

2-O-Benzoyllycorine

2

> 50

> 50

1,2-O,O'-Di-trans-cinnamoyllycorine

3

46.76 ± 0.95

17.45 ± 0.19

2-O-trans-Cinnamoyllycorine

4

> 50

19.74 ± 1.37

1-O-trans-Cinnamoyllycorine

5

> 50

12.13 ± 0.77

1-O-Acetyl-2-O-tert-butyldimethylsilyllycorine

6

> 50

> 50

2-O-tert-Butyldimethylsilyl-1-O-(methylthio)methyllycorine

7

11.40 ± 0.66

4.17 ± 0.29

Lycorin-2-one

8

> 50

> 50

1-O-Acetyllycorin-2-one

9

> 50

44.46 ± 0.88

1-O-trans-Cinnamoyllycorin-2-one

10

> 50

20.91 ± 0.13

Tacrine (positive control)

 

0.26 ± 0.015

0.02 ± 0.00

Galanthamine (positive control)

 

1.60 ± 0.14

18.30 ± 0.14