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Table 2 The anti-AChE and anti-BChE activity of 4a-m derivatives[a]

From: Amino-7,8-dihydro-4H-chromenone derivatives as potential inhibitors of acetylcholinesterase and butyrylcholinesterase for Alzheimer’s disease management; in vitro and in silico study

Entry

R1

R2

R3

ACHE % Inhibition at 50 µM

BChE % Inhibition at 50 µM

BChE (IC50, µM)

4a

H

H

H

21.02 ± 1.31

39.77 ± 1.39

4b

–NO2

H

H

28.89 ± 2.56*

58.72 ± 1.18

27.42 ± 2.01

4c

H

H

23.57 ± 1.20

77.67 ± 3.77

0.89 ± 0.24

4d

H

H

23.42 ± 1.00

67.82 ± 1.70

1.19 ± 0.31

4e

H

H

34.44 ± 3.10*

58.94 ± 0.93

26.35 ± 3.34

4f

H

H

4.42 ± 0.57*

61.96 ± 7.24

5.70 ± 0.68

4g

H

H

14.97 ± 2.59*

57.29 ± 9.75

13.06 ± 2.59

4h

H

H

7.35 ± 0.56*

21.3 ± 2.69

4i

H

H

19.45 ± 2.39

42.79 ± 1.22

4j

H

H

16.34 ± 0.63*

38.28 ± 4.36

4k

OCH3

H

41.07 ± 2.33*

80.47 ± 5.08

0.65 ± 0.13

4l

OCH3

H

33.59 ± 3.29*

76.12 ± 0.88

2.63 ± 0.19

4m

OCH3

H

12.91 ± 1.27*

69.65 ± 1.52

1.51 ± 0.20

  1. [a]Data present here are the mean ± S.E (Table S1) and donepezil as postive control exhibited IC50 = 0.079 ± 0.05 µM against AChE and IC50 = 10.6 ± 2.1 µM against BChE
  2. *Indicates a significant difference (P < 0.05) in comparison between 4a as unsubstituted derivatives compared with the rest of the compounds in the AChE set
  3. Indicates significant differences (P < 0.05) in comparison between 4a as unsubstituted derivatives compared with the rest of the compounds in the BChE set