Table 2.
Comp. | R | N‐alkyl | AChE (μ m)a | BChE (μ m)a | SIb |
---|---|---|---|---|---|
4aa | H | CH2=CHCH2 | 211.72 ± 0.02 | 456.95 ± 0.03 | 2.16 |
4ab | CH3 | CH2=CHCH2 | 75.17 ± 0.01 | 31.66 ± 0.01 | 0.42 |
4ac | OCH3 | CH2=CHCH2 | 75.10 ± 0.01 | 62.23 ± 0.02 | 0.83 |
4ad | Cl | CH2=CHCH2 | 293.52 ± 0.02 | 62.26 ± 0.08 | 0.21 |
4ae | CH2CH3 | CH2=CHCH2 | 173.96 ± 0.02 | 25.58 ± 0.02 | 0.15 |
4af | F | CH2=CHCH2 | 72.91 ± 0.01 | 135.29 ± 0.02 | 1.86 |
4ag | Br | CH2=CHCH2 | 168.03 ± 0.06 | 29.08 ± 0.03 | 0.17 |
4ba | H | HC≡CCH2 | 421.30 ± 0.03 | 896.70 ± 0.03 | 2.13 |
4bb | CH3 | HC≡CCH2 | 259.63 ± 0.01 | 455.59 ± 0.01 | 1.75 |
4bc | OCH3 | HC≡CCH2 | 412.69 ± 0.01 | 1206.84 ± 0.01 | 2.92 |
4bd | Cl | HC≡CCH2 | 392.91 ± 0.04 | 1327.55 ± 0.17 | 3.38 |
4be | CH2CH3 | HC≡CCH2 | 443.66 ± 0.01 | 1976.73 ± 0.09 | 4.46 |
4bf | F | HC≡CCH2 | 375.61 ± 0.03 | 894.37 ± 0.03 | 2.38 |
4bg | Br | HC≡CCH2 | 661.38 ± 0.09 | 894.77 ± 0.06 | 1.35 |
Galantamine | – | – | 0.54 ± 0.7 | 8.80 ± 0.5 | 16.29 |
Values are the average from three independent experiments.
Selectivity for AChE is defined as IC50 (BChE)/IC50 (AChE).