Pharmacological Evaluation and Docking Studies of 3-Thiadiazolyl- and Thioxo-1,2,4-triazolylcoumarin Derivatives as Cholinesterase Inhibitors
Table 1
AChE and BuChE inhibitory activities of new coumarin derivativesa.
Code
Compound
EeAChE
rAChE
hBChE
rBChE
R
SEM [μM]
3a
2-Cl
2.42 ± 0.43
0.47 ± 0.07
0.19 ± 0.01
21.4 ± 1.6
3b
3-Cl
0.32 ± 0.07
0.60 ± 0.03
0.036 ± 0.003
65.7 ± 2.0
3c
4-Cl
0.45 ± 0.09
0.013 ± 0.002
1.34 ± 0.02
0.52 ± 0.03
3d
3-CH3
5.77 ± 0.31
0.082 ± 0.002
0.18 ± 0.02
1.11 ± 0.05
3e
4-CH3
18.4 ± 3.4
0.039 ± 0.002
0.13 ± 0.01
0.14 ± 0.05
3f
2-OCH3
4.06 ± 0.34
0.061 ± 0.005
0.28 ± 0.01
0.69 ± 0.02
3g
3-OCH3
0.98 ± 0.34
0.046 ± 0.002
7.55 ± 0.03
22.1 ± 0.2
4a
2-Cl
5.75 ± 0.78
0.031 ± 0.008
0.10 ± 0.01
1.39 ± 0.02
4b
3-Cl
0.28 ± 0.07
0.028 ± 0.002
0.54 ± 0.09
2.26 ± 0.02
4c
4-Cl
48.6 ± 4.4
0.240 ± 0.021
0.42 ± 0.01
0.35 ± 0.01
4d
3-CH3
28.01 ± 1.63
0.017 ± 0.002
0.66 ± 0.01
0.51 ± 0.01
4e
4-CH3
6.19 ± 0.29
0.561 ± 0.022
0.28 ± 0.02
0.46 ± 0.01
4f
2-OCH3
7.16 ± 0.01
0.081 ± 0.001
0.23 ± 0.01
1.36 ± 0.03
4g
3-OCH3
8.26 ± 0.01
0.021 ± 0.001
0.34 ± 0.01
1.52 ± 0.03
Neostigmine
0.056 ± 0.006
0.048 ± 0.003
0.06 ± 0.005
0.047 ± 0.006
Donepezil
0.023 ± 0.003
n.d
6.18 ± 0.34
n.d
aValues are expressed as the mean ± standard error of the mean of three experiments. inhibitory concentration (μM) of AChE from electrophorus electricus (EeAChE) or rabbit (rAChE) and (hBChE) from horse serum or rabbit serum (rBChE).