Table 1.
The chemical structures and biological activities of DL0410 and its 50 derivatives as AChE and BuChE inhibitors.
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Compound No. | R1 | R2 | IC50(μM) | |
AChE | BuChE | |||
1-1 | ![]() |
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0.096 | 1.25 |
1-2 | ![]() |
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0.84 | 2.22 |
1-3 | ![]() |
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1.32 | 5.9 |
1-4 | ![]() |
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0.82 | 2.65 |
1-5 | ![]() |
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0.41 | 1.88 |
1-6 | ![]() |
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3.32 | 4.87 |
1-7 | ![]() |
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49.05 | 36.58 |
1-8 | ![]() |
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0.75 | 0.19 |
1-9 | ![]() |
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1.18 | 0.74 |
1-10 | ![]() |
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0.88 | 2.83 |
1-11 | ![]() |
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0.71 | 2.39 |
1-12 | ![]() |
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0.33 | 1.16 |
1-13 | ![]() |
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1.43 | 1.94 |
1-14 | ![]() |
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1.61 | 13.77 |
1-15 | ![]() |
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0.97 | 0.72 |
1-16 | ![]() |
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2.15 | 1.91 |
1-17 | ![]() |
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3.33 | 6.56 |
1-18 | ![]() |
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9.52 | >200 |
1-19 | ![]() |
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0.25 | >200 |
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Compound No. | R1 | R2 | IC50(μM) | |
AChE | BuChE | |||
2-1 | ![]() |
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75.54 | 20.72 |
2-2 | ![]() |
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74.13 | 66.51 |
2-3 | ![]() |
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0.50 | 3.41 |
2-4 | ![]() |
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3.67 | 19.18 |
2-5 | ![]() |
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0.19 | 1.64 |
2-6 | ![]() |
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12.24 | >200 |
2-7 | ![]() |
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3.53 | 6.38 |
2-8 | ![]() |
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62.27 | 9.11 |
2-9 | ![]() |
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2.62 | 1.21 |
2-10 | ![]() |
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3.96 | 2.77 |
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Compound No. | R1 | R2 | IC50(μM) | |
AChE | BuChE | |||
3-1 | ![]() |
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4.11 | 4.2 |
3-2 | ![]() |
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7.09 | 7.65 |
3-3 | ![]() |
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48.53 | 40.00 |
3-4 | ![]() |
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7.55 | 24.35 |
3-5 | ![]() |
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3.32 | 1.72 |
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Compound No. | R1 | R2 | IC50(μM) | |
AChE | BuChE | |||
4-1 | ![]() |
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4.89 | 6.00 |
4-2 | ![]() |
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54.44 | 5.95 |
4-3 | ![]() |
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3.07 | 3.09 |
4-4 | ![]() |
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17.40 | 2.93 |
4-5 | ![]() |
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15.67 | 16.32 |
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Compound No. | R | IC50(μM) | ||
AChE | BuChE | |||
5-1 | O | 0.89 | 5.68 | |
5-2 | S | 3.89 | 3.44 | |
5-3 | ![]() |
14.08 | >200 | |
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Compound No. | R | IC50(μM) | ||
AChE | BuChE | |||
6-1 | O | 0.06 | 0.61 | |
6-2 | S | 2.03 | 1.71 | |
Compound No. | Structure | IC50(μM) | ||
AChE | BuChE | |||
7-1 | ![]() |
31.74 | 13.78 | |
7-2 | ![]() |
17.13 | 1.55 | |
7-3 | ![]() |
34.09 | 0.06 | |
7-4 | ![]() |
18.53 | >200 | |
7-5 | ![]() |
3.35 | 0.20 | |
7-6 | ![]() |
0.03 | 0.44 | |
7-7 | ![]() |
1.42 | 4.79 |