Table 1 Inhibitions of hMAO-A and hMAO-B by B series.

From: Introduction of benzyloxy pharmacophore into aryl/heteroaryl chalcone motifs as a new class of monoamine oxidase B inhibitors

Compounds

Residual activity at 10 µM (%)

IC50 (µM)

SIa

hMAO-A

hMAO-B

hMAO-A

hMAO-B

B1

82.62 ± 5.03

35.53 ± 6.05

26.923 ± 4.160

1.441 ± 0.149

18.677

B2

53.15 ± 1.58

23.59 ± 0.96

13.728 ± 1.531

0.626 ± 0.296

21.933

B3

58.32 ± 0.84

0

14.267 ± 0.203

0.261 ± 0.016

54.663

B4

78.25 ± 4.32

16.24 ± 6.49

29.376 ± 2.708

0.233 ± 0.110

125.915

B5

89.21 ± 4.47

0

 > 40

0.224 ± 0.082

 > 178.651

B6

92.00 ± 2.93

41.33 ± 4.90

 > 40

6.550 ± 1.344

 > 6.107

B7

58.43 ± 4.48

0

12.597 ± 0.898

0.149 ± 0.006

84.544

B8

92.45 ± 0.49

64.36 ± 1.50

 > 40

17.880 ± 0.268

 > 2.237

B9

69.09 ± 1.54

0

23.966 ± 1.443

0.236 ± 0.017

101.551

B10

76.67 ± 3.22

0

33.821 ± 6.888

0.067 ± 0.005

504.791

B11

81.27 ± 2.92

41.20 ± 0.12

 > 40

5.784 ± 2.387

 > 6.915

B12

86.70 ± 2.68

75.44 ± 3.60

 > 40

37.559 ± 1.882

 > 1.065

B13

99.12 ± 1.24

1.39 ± 3.27

 > 40

0.255 ± 0.016

 > 156.617

B14

91.23 ± 6.20

51.85 ± 1.31

 > 40

11.347 ± 0.331

 > 3.525

B15

75.88 ± 3.10

0

34.512 ± 3.544

0.120 ± 0.010

287.600

Toloxatone

  

1.080 ± 0.025

–

 

Lazabemide

  

–

0.110 ± 0.016

 

Clorgyline

  

0.007 ± 0.0007

–

 

Pargyline

  

–

0.140 ± 0.0059

 
  1. Results are the means ± standard errors of duplicate or triplicate experiments.
  2. aSelectivity index (SI) values are expressed for hMAO-B as compared with hMAO-A.
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