Table 2. Acetylcholinesterase inhibitory activities of studied chalcone compounds
|
Compounds | A-ring | B-ring | IC50 |
R’1 | R’2 | R’3 | R1 | R2 | R3 | R4 | (μg/ml) | (μM) | r2* |
S1 | OH | H | H | Cl | H | H | H | 23.81 | 92.42 | 0.97 |
S2 | OH | H | H | H | H | Cl | H | 13.62 | 52.71 | 0.93 |
S3 | OH | H | H | Cl | H | Cl | H | 14.91 | 51.01 | 0.89 |
S4 | OH | H | H | Cl | Cl | H | H | 18.32 | 62.37 | 0.85 |
S5 | OH | H | H | OMe | H | OMe | H | 24.63 | 86.45 | 0.84 |
S6 | OH | H | H | OMe | OMe | H | H | > 100 | ND | ND |
S7 | OH | H | H | H | OMe | OMe | OMe | > 100 | ND | ND |
S8 | OH | H | H | H | H | N(Me)2 | H | > 100 | ND | ND |
S9 | OH | OMe | H | OMe | OMe | H | H | 60.12 | 190.98 | 0.90 |
S10 | OH | OMe | H | H | OMe | OMe | H | 40.80 | 129.90 | 0.99 |
S11 | OH | OMe | H | H | OMe | OMe | OMe | > 100 | > 250 | ND |
S12 | OH | OMe | H | H | H | Cl | H | > 100 | > 250 | ND |
S13 | OH | OMe | OMe | OMe | H | OMe | H | > 100 | > 250 | ND |
S14 | OH | OMe | OMe | H | OMe | OMe | H | > 100 | > 250 | ND |
S15 | OH | OMe | OMe | OMe | OMe | OMe | H | > 100 | > 250 | ND |
S16 | OH | OMe | OMe | H | H | Cl | H | 67.88 | 213.14 | 0.95 |
S17 | H | NH2 | H | Cl | H | H | H | 9.32 | 36.10 | 0.88 |
S18 | H | NH2 | H | H | H | Cl | H | > 100 | > 250 | ND |
S19 | H | NH2 | H | H | H | NO2 | H | > 100 | > 250 | ND |
S20 | H | NO2 | H | H | H | N(Me)2 | H | > 100 | > 250 | ND |
Chalcone | H | H | H | H | H | H | H | > 100 | > 250 | ND |
Galantamine** | | | | | | | | 1.36 | 0.4 | 0.93 |
Coefficient of determination of the regression line indicating the correlation between common logarithm of the concentrations of investigated compounds (μM) and their percentages of AChE inhibition (%);
: used as control substance; ND: Not detected