Skip to main content
. 2021 Jul 26;6(30):19924–19939. doi: 10.1021/acsomega.1c02875

Table 3. In Vitro Inhibitory Activity of Compounds 1–17 toward Cholinesterases.

graphic file with name ao1c02875_0010.jpg

          cholinesterase IC50 (μM)a
  
compound R1 R2 R3 R4 eeAChEb eqBChEc SId
1 H H H H 0.03 ± 0.00 68.78 ± 03.15 2,273
2 Br H H H 2.56 ± 0.17 72.29 ± 04.57 28
3 I H H H 14.12 ± 0.84 325.22 ± 38.63 23
4 F H H H 1.23 ± 0.01 63.998 ± 03.63 52
5 Me H H H 0.35 ± 0.02 486.03 ± 29.71 1,388
6 Et H H H 0.57 ± 0.09 60.39 ± 02.54 105
7 CN H H H 33.88 ± 1.95 1,050.88 ± 498.89 31
8 NH2 H H H 0.32 ± 0.01 524.64 ± 41.56 1,634
9 OH H H H 0.53 ± 0.09 154.76 ± 04.14 293
10 OMe H H H 0.16 ± 0.02 599.15 ± 49.76 3,633
11 OEt H H H 0.22 ± 0.04 253.02 ± 12.24 1,154
12 OnPr H H H 10.19 ± 0.50 87.27 ± 01.37 9
13 OnBu H H H 109.65 ± 9.59 16.91 ± 01.23 0.2
14     H H 3.67 ± 0.28 903.66 ± 88.20 246
15     Me Me n.i. 1,348.75 ± 62.31  
16   Me Me Me n.i. 258.70 ± 10.81  
17     Me Me 0.61 ± 0.02 223.57 ± 47.78 366
donepezile         0.23 ± 0.05 18.00 ± 00.79 79
a

Mean IC50 (μM) ± SEM, n = 3; n.i. = no inhibition.

b

AChE (EC 3.1.1.7) from electric eel.

c

BChE (EC 3.1.1.8) from horse serum.

d

Selectivity index for AChE is defined as IC50 (BChE)/IC50 (AChE).

e

Donepezil, a known selective AChE inhibitor used as a positive control.29