Table 1.
Cpd | Log P | BACE1 | Anti-Aβ aggregation | Fe chelation | DPPH | ||||
---|---|---|---|---|---|---|---|---|---|
| |||||||||
% Inhibition (at 25 μM) (±SEM) | IC50 (μM) | % Inhibition (at 100 μM) (±SEM) | IC50 (μM) | % Capacity (at 100 μM) (±SEM) | Stoichiometric ratio (Fe:cpd) | % Inhibition (at 100 μM) (±SEM) | IC50 (μM) | ||
6a | 4.69 | 67.95 (±0.35) | 19.82 | NA | - | 9.67 (±0.32) | - | NA | - |
6ba | 3.86 | 73.63 (±1.47) | 18.86 | 7.19 (±1.19) | - | 12.35 (±0.68) | - | NA | - |
6c | 4.10 | 78.91 (±2.83) | 18.03 | 10.12 (±0.86) | - | 15.88 (±0.21) | - | NA | - |
6d | 3.01 | 14.10 (±1.79) | - | NA | - | 32.86 (±0.19) | - | 2.81 (±0.37) | - |
6e | 2.16 | 12.57 (±1.10) | - | NA | - | 20.63 (±0.35) | - | 5.45 (±0.33) | - |
6f | 1.41 | 21.28 (±1.92) | - | NA | - | 5.80 (±0.04) | - | NA | - |
6g | 2.01 | 21.14 (±1.13) | - | 66.36 (±2.02) | 82.90 | 8.88 (±0.25) | - | 47.03 (±0.12) | 106.41 |
| |||||||||
6h | 1.75 | 21.72 (±0.33) | - | 84.13 (±2.49) | 29.86 | 42.74 (±0.30) | 1:3 | 92.29 (±0.02) | 42.91 |
| |||||||||
12a | 4.42 | 18.91 (±0.40) | - | 17.81 (±0.86) | - | 42.65 (±1.07) | - | NA | - |
12b | 3.58 | 30.42 (±3.54) | - | 34.02 (±10.13) | - | 10.54 (±0.22) | - | NA | - |
| |||||||||
12c | 3.83 | 61.46 (±1.83) | 20.75 | 67.56 (±0.72) | 83.23 | 60.90 (±0.51) | 1:3 | NA | - |
| |||||||||
12d | 2.73 | 32.97 (±0.37) | - | 82.52 (±1.26) | 47.51 | 13.87 (±0.59) | - | 1.56 (±0.51) | - |
12e | 1.88 | 7.53 (±1.79) | - | 36.03 (±1.92) | - | 41.42 (±1.13) | - | NA | - |
12f | 1.13 | 16.57 (±2.91) | - | 3.80 (±1.56) | - | 13.06 (±0.16) | - | 1.32 (±0.78) | - |
12g | 1.74 | 16.23 (±0.45) | - | 46.06 (±1.63) | 109.83 | 77.70 (±0.67) | 1:3 | 40.79 (±0.31) | 130.44 |
| |||||||||
12h | 1.47 | 40.03 (±0.95) | - | 81.48 (±2.54) | 56.39 | 66.45 (±0.37) | 1:3 | 50.58 (±0.17) | 92.70 |
| |||||||||
Inh IV (Merck®) | 1.23 | 96.51 (±1.33) | 0.015b | - | - | - | - | - | - |
Curcumin | 2.56 | - | - | 82.90 (±0.82) | 0.63c | - | - | - | - |
EDTA | −2.69 | - | - | - | - | 98.00 (±0.34) | - | - | |
Ascorbic acid | −3.36 | - | - | - | - | - | - | 53.64 (±0.11) | 94.92 |