TABLE 1.
Compounds | Position | R | IC50a (μmol/L)
|
Selectivity for AChEb | |
---|---|---|---|---|---|
AChE | BChE | ||||
5d | Para | 0.37 ± 0.03 | >500 | >1340 | |
6d | Meta | 0.92 ± 0.07 | 15.32 ± 1.16 | 16.64 | |
7d | Ortho | 16.40 ± 0.22 | 15.16 ± 0.60 | 0.92 | |
9d | Para | 18.61±1.06 | >500 | >26.86 | |
10d | Meta | >500 | 44.02±2.37 | <0.09 | |
11d | Ortho | >500 | >500 | - | |
12k | Para | 1.65±0.09 | 8.48±0.29 | 5.15 | |
13k | Para | 7.07 ± 0.46 | 13.22 ± 0.32 | 1.87 | |
| |||||
5e | Para | 0.15 ± 0.01 | 4.11 ± 0.16 | 27.40 | |
6e | Meta | 3.25 ± 0.14 | 4.62 ±0.16 | 1.42 | |
7e | Ortho | 230.34±14.82 | 3.76±0.35 | 0.02 | |
9e | Para | >500 | >500 | - | |
10e | Meta | >500 | >500 | - | |
11e | Ortho | >500 | >500 | - | |
12l | Para | 1.67±0.04 | 0.46±0.01 | 0.28 | |
13l | Para | 28.95 ± 1.68 | 13.61 ± 0.53 | 0.47 | |
| |||||
5f | Para | 0.69 ± 0.06 | 1.03 ± 0.05 | 1.49 | |
6f | Meta | 0.61 ± 0.02 | 4.01 ± 0.14 | 6.61 | |
7f | Ortho | 29.86 ± 0.98 | 4.50 ± 0.22 | 0.15 | |
9f | Para | >500 | >500 | - | |
10f | Meta | 152.49±12.82 | 222.84±11.54 | 1.46 | |
11f | Ortho | >500 | 106.14±3.09 | 0.21 | |
12m | Para | 0.37±0.02 | 0.52±0.01 | 1.41 | |
13m | Para | 9.58 ± 0.80 | 6.41 ± 0.36 | 0.67 | |
| |||||
5g | Para | 4.34 ± 0.29 | 6.21 ±0.19 | 1.43 | |
6g | Meta | 51.30 ± 1.04 | 1.12 ± 0.11 | 0.02 | |
7g | Ortho | 202.70 ± 2.50 | 1.96 ± 0.14 | 0.01 | |
| |||||
5h | Para | >500 | >500 | - | |
6h | Meta | >500 | >500 | - | |
7h | Ortho | 260.95±4.17 | 28.98±1.23 | 0.11 | |
| |||||
5i | Para | >500 | >500 | - | |
6i | Meta | >500 | >500 | - | |
7i | Ortho | >500 | >500 | - | |
| |||||
5j | Para | >500 | >500 | - | |
6j | Meta | >500 | >500 | - | |
7j | Ortho | >500 | 100.33±6.84 | <0.20 | |
| |||||
Rivastigmine* | 10.54±0.86 | 0.26±0.08 | 0.02 |
IC50: 50% inhibitory concentration (means±SD of three assays).
Selectivity for AChE is defined as IC50 (BChE)/IC50 (AChE).
Used for control.