Research Article

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.

707932.tab.001

CodeCompoundEeAChErAChEhBChErBChE
R 𝐾 𝑖 ± SEM [μM]

3a2-Cl2.42 ± 0.430.47 ± 0.070.19 ± 0.0121.4 ± 1.6
3b3-Cl0.32 ± 0.070.60 ± 0.030.036 ± 0.00365.7 ± 2.0
3c4-Cl0.45 ± 0.090.013 ± 0.0021.34 ± 0.020.52 ± 0.03
3d3-CH35.77 ± 0.310.082 ± 0.0020.18 ± 0.021.11 ± 0.05
3e4-CH318.4 ± 3.40.039 ± 0.0020.13 ± 0.010.14 ± 0.05
3f2-OCH34.06 ± 0.340.061 ± 0.0050.28 ± 0.010.69 ± 0.02
3g3-OCH30.98 ± 0.340.046 ± 0.0027.55 ± 0.0322.1 ± 0.2
4a2-Cl5.75 ± 0.780.031 ± 0.0080.10 ± 0.011.39 ± 0.02
4b3-Cl0.28 ± 0.070.028 ± 0.0020.54 ± 0.092.26 ± 0.02
4c4-Cl48.6 ± 4.40.240 ± 0.0210.42 ± 0.010.35 ± 0.01
4d3-CH328.01 ± 1.630.017 ± 0.0020.66 ± 0.010.51 ± 0.01
4e4-CH36.19 ± 0.290.561 ± 0.0220.28 ± 0.020.46 ± 0.01
4f2-OCH37.16 ± 0.010.081 ± 0.0010.23 ± 0.011.36 ± 0.03
4g3-OCH38.26 ± 0.010.021 ± 0.0010.34 ± 0.011.52 ± 0.03
Neostigmine0.056 ± 0.0060.048 ± 0.0030.06 ± 0.0050.047 ± 0.006
Donepezil0.023 ± 0.003n.d6.18 ± 0.34n.d

aValues are expressed as the mean ± standard error of the mean of three experiments. 𝐾 𝑖 inhibitory concentration (μM) of AChE from electrophorus electricus (EeAChE) or rabbit (rAChE) and (hBChE) from horse serum or rabbit serum (rBChE).