Table 1.
AbTYR inhibitory effects 7–32, 5 a–c and kojic acid (KA)
|
Compd |
n |
R1 |
R2 |
Diphenolase activity IC50 [μM][a] |
|---|---|---|---|---|
|
5 a |
0 |
H |
H |
13.34±0.73 |
|
5 b |
0 |
2‐CF3 |
H |
0.48±0.05 |
|
5 c |
0 |
2,4‐(NO2)2 |
H |
0.96±0.21 |
|
7 |
1 |
H |
H |
4.28±0.86 |
|
8 |
2 |
H |
H |
13.17±2.71 |
|
9 |
1 |
H |
Ph |
40.43±0.81 |
|
10 |
1 |
2‐Cl |
H |
8.70±0.86 |
|
11 |
1 |
3‐Cl |
H |
4.66±0.89 |
|
12 |
1 |
4‐Cl |
H |
4.71±0.63 |
|
13 |
1 |
2‐Br |
H |
4.70±0.65 |
|
14 |
1 |
3‐Br |
H |
15.74±0.69 |
|
15 |
1 |
4‐Br |
H |
7.66±0.42 |
|
16 |
1 |
2‐NO2 |
H |
8.31±1.56 |
|
17 |
1 |
3‐NO2 |
H |
8.66±0.78 |
|
18 |
1 |
4‐NO2 |
H |
1.71±0.79 |
|
19 |
1 |
4‐OMe |
H |
19.63±1.58 |
|
20 |
1 |
2‐NH2 |
H |
3.74±0.54 |
|
21 |
1 |
3‐NH2 |
H |
9.36±0.45 |
|
22 |
1 |
4‐NH2 |
H |
16.73±0.57 |
|
23 |
0 |
2‐CF3,3−F |
H |
0.45±0.03 |
|
24 |
0 |
2‐CF3,4−F |
H |
0.87±0.01 |
|
25 |
0 |
2‐CF3,5−F |
H |
0.24±0.03 |
|
26 |
0 |
2‐NO2,3−Cl |
H |
0.18±0.03 |
|
27 |
0 |
2‐NO2,4−Cl |
H |
2.27±0.49 |
|
28 |
0 |
2‐NO2,5−Cl |
H |
2.01±0.23 |
|
29 |
0 |
2‐NO2,6−Cl |
H |
1.17±0.18 |
|
30 |
0 |
2‐NO2,3−OMe |
H |
2.09±0.27 |
|
31 |
0 |
2‐NO2,4−OMe |
H |
1.80±0.13 |
|
32 |
0 |
2‐NO2,5−OMe |
H |
1.11±0.09 |
|
KA |
– |
– |
– |
17.76±0.18 |
[a] IC50: concentration that caused 50 % enzyme activity loss. The mean value and standard deviation were calculated from triplicate experiments.