Group 1
Compound Side chain (R) % Inhibition AChEa % Inhibition BChEa
1 n=2, R=C2H5 30.4 ± 6.0 83.9 ± 1.5
2 n=3, R=CH3 32.6 ± 3.4 63.5 ± 4.6
3 n=3, R=C2H5 47.4 ± 3.9 66.3 ± 0.4
4 n=4, R=C2H5 65.5 ± 1.0 79.5 ± 1.0
Group 2
Compound Side chain (R) % Inhibition AChEa % Inhibition BChEa
5 2’-N(CH3)2 34.9 ± 1.4 48.0 ± 9.9
6 3’-N(CH3)2 18.4 ± 7.6 86.3 ± 1.2
7 4’-N(CH3)2 50.6 ± 2.8 57.1 ± 4.6
8 3’-N(C2H5)2 31.7 ± 1.8 51.6 ± 5.4
9 4’-N(C2H5)2 64.1 ± 0.9 55.9 ± 2.7
10 3’- 23.3 ± 2.6 80.5 ± 1.6
11 3’- 63.8 ± 2.8 65.6 ± 7.7
12 4’- 52.3 ± 2.8 38.6 ± 0.9
13 3’- 28.3 ± 8.5 68.3 ± 2.7
14 4’- 8.4 ± 5.2 19.6 ± 4.9
15 3’- 25.1 ± 1.0 50.7 ± 2.4
16 4’- 54.4 ± 0.4 51.3 ± 1.7
17 52.0 ± 4.9 68.3 ± 2.7
18 NDb NDb
19 43.7 ± 2.7 10.2 ± 7.9
20 23.7 ± 5.7 14.7 ± 0.7
21 30.4 ± 3.9 6.5 ± 4.9
22 49.6 ± 1.9 25.1 ± 5.6
23 28.5 ± 4.3 35.3 ± 0.2
24 62.1 ± 0.3 79.6 ± 0.8
25 H 40.9 ± 5.0 30.5 ± 4.5
26 4’-CN 19.2 ± 2.2 -1.7 ± 3.4
27 4’-F 45.8 ± 6.4 0.7 ± 0.9
28 3’,4’-diF 47.2 ± 7.6 -4.6 ± 5.6
29 4’-OCH3 46.4 ± 9.8 31.3 ± 4.4
30 3’-OH 5.3 ± 4.7 -3.6 ± 1.6
31 3’,4’-diOH 47.4 ± 4.0 -1.7 ± 3.8
Group 3
Compound Side chain (R) % Inhibition AChEa % Inhibition BChEa
32 n=1, R=H 69.1 ± 3.1 41.9 ± 3.3
33 n=1, R=CH3 38.3 ± 1.9 12.8 ± 3.8
34 n=1, R=Cl 64.9 ± 4.9 32.8 ± 3.1
35 n=1, R=OCH3 34.3 ± 2.1 8.6 ± 5.0
36 n=1, R=CN 34.0 ± 3.8 35.5 ± 0.9
37 n=2, R=H 67.8 ± 1.0 38.7 ± 0.6
38 n=2, R=CH3 71.1 ± 5.3 36.7 ± 2.5
39 n=2, R=Cl 78.5 ± 0.2 30.5 ± 5.1
40 n=2, R=OCH3 82.0 ± 1.6 20.9 ± 1.5
41 n=3, R=H 95.6 ± 0.7 37.1 ± 5.8
Group 4
 
Compound Side chain (R) % Inhibition AChEa % Inhibition BChEa
42 59.2 ± 4.9 20.6 ± 4.0
43 52.5 ± 2.0 59.5 ± 1.0
44 -OPh NDb NDb
45 46.0 ± 6.7 1.4 ± 0.4
46 -NH2 NDb NDb
Group 5
Compound Side chain (R) % Inhibition AChEa % Inhibition BChEa
47 H 92.5 ± 0.4 99.7 ± 0.4
48 47.6 ± 7.1 86.5 ± 1.9
Group 6
Compound Side chain (R) % Inhibition AChEa % Inhibition BChEa
49 H 97.9 ± 0.3 98.0 ± 0.3
50 97.0 ± 0.1 95.3 ± 0.4
51 97.8 ± 0.1 88.4 ± 0.8
52 82.1 ± 1.3 34.6 ± 5.3
53 81.6 ± 3.0 50.7 ± 5.7
54 77.7 ± 1.0 42.9 ± 2.9
Group 7
Compound Side chain (R) % Inhibition AChEa % Inhibition BChEa
55 H 0.4 ± 5.4 2.0 ± 0.5
56 6.6 ± 1.4 4.4 ± 1.3
57 54.0 ± 4.3 7.6 ± 2.6
58 15.4 ± 4.8 7.0 ± 0.6
59 6.2 ± 5.8 4.1 ± 1.7
60 31.9 ± 2.2 6.4 ± 1.7
a :% Inhibition is presented as mean ± SEM from 3 independent determinations.
b: Not determined
Table 1: Percent inhibition of AChE and BChE by compounds in Groups 1-7 tested
at a fixed concentration of 3µM.