Table 2 Inhibition of AChE and BuChE activities of title compounds

Compd.

R³

IC₅₀ (μM) ^a for AChE

IC₅₀ (μM) for BuChE

Selectivity for BuChE/AChE

1a

H

106.72 ± 5.78

62.93 ± 0.84

0.59

1b

H

73.72 ± 1.36

36.98 ± 0.56

0.50

1c

H

81.92 ± 2.04

35.49 ± 1.68

0.43

1d

H

79.34 ± 5.78

42.98 ± 1.76

0.54

1e

H

95.35 ± 1.70

>100

>1.05

2a

CH₃

2.34 ± 0.20

10.89 ± 0.20

4.66

2b

CH₃

2.40 ± 0.49

6.79 ± 0.56

2.83

2c

CH₃

4.20 ± 0.29

7.21 ± 0.75

1.72

2d

CH₃

7.00 ± 0.07

10.62 ± 0.22

1.53

2e

CH₃

7.76 ± 2.36

>100

>12.89

3a

5.84 ± 1.19

4.66 ± 0.64

0.80

3b

6.00 ± 0.33

1.54 ± 0.14

0.26

3c

4.36 ± 0.58

3.05 ± 0.13

0.70

3d

3.70 ± 0.16

1.73 ± 0.08

0.47

3e

74.73 ± 4.07

>100

>1.34

4a

2.63 ± 0.07

1.49 ± 0.03

0.57

4b

2.60 ± 0.13

0.51 ± 0.01

0.20

4c

5.85 ± 0.32

2.89 ± 0.07

0.49

4d

55.34 ± 8.15

5.61 ± 0.08

0.10

4e

24.16 ± 0.40

8.83 ± 0.36

0.37

Galanthamine · HBr

1.12 ± 0.02

29.99 ± 0.05

26.78