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Applied Biological Chemistry

Table 1 Inhibitions of MAO-A and MAO-B by chalcone derivatives

From: Development of morpholine ring-bearing halogenated α,β-unsaturated ketones as selective monoamine oxidase-B inhibitors

Compound

Residual activity (%)

IC50 (μM)

SI

MAO-A (10 μM)

MAO-B (1 μM)

MAO-A

MAO-B

MHC1

51.15 ± 0.87

4.35 ± 1.44

11.97 ± 0.27

0.21 ± 0.010

57.00

MHC2

26.14 ± 2.55

19.74 ± 7.44

0.82 ± 0.25

0.13 ± 0.01

6.31

MHC3

50.56 ± 2.21

23.42 ± 6.41

11.67 ± 1.38

0.17 ± 0.04

68.65

MHC4

28.16 ± 4.06

−7.98 ± 3.76

7.61 ± 0.19

0.095 ± 0.012

80.11

MHC5

23.55 ± 2.42

0.02 ± 1.55

4.30 ± 0.043

0.065 ± 0.014

66.15

MHC6

15.47 ± 5.50

7.10 ± 0.61

3.04 ± 0.068

0.082 ± 0.012

37.07

MHC7

24.63 ± 3.59

−3.11 ± 1.89

2.89 ± 0.62

0.078 ± 0.007

37.05

MHC8

72.93 ± 1.68

7.20 ± 2.33

15.37 ± 0.81

0.15 ± 0.02

102.47

MHC9

20.28 ± 2.06

−1.60 ± 2.26

4.28 ± 0.052

0.13 ± 0.05

32.92

Toloxatone

–

–

1.65 ± 0.094

 > 40

0.041

Safinamide

–

–

 > 40

0.019 ± 0.0019

2105.26

Clorgyline

–

–

0.008 ± 0.001

2.43 ± 0.71

0.0033

Pargyline

–

–

2.15 ± 0.23

0.11 ± 0.01

19.55

  1. Data were analyzed with independent duplicate or triplicate experiments and presented as the means ± standard error. The selectivity index (SI) was expressed for MAO-B using IC50 values, that is, IC50 of MAO-A/ IC50 of MAO-B
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