Structural data and inhibitory activities of compounds 1–5 against human AChE and equine BuChE.
Compound | R1 | R2 | Human AChE IC50/μMa | equine BuChE IC50/μMa | Selectivity for BuChEc |
---|---|---|---|---|---|
1 | Br | H | 10.5 ± 2.9 | 5.7 ± 1.0 | 1.8 |
2 | Cl | H | 14.5 ± 5.8 | 4.6 ± 1.0 | 3.2 |
3 | Br | OCH3 | 19.5 ± 6.0 | 11.9 ± 2.0 | 1.6 |
4 | OCH3 | H | 32.3 ± 5.3 | 4.0 ± 0.8 | 8.1 |
5 | NO2 | H | 14.2 ± 2.3 | 17.8 ± 2.0 | 0.8 |
Donepezilb | 0.09 ± 0.01 | 1.9 ± 0.2 | 0.05 | ||
Propidiumb | 11 ± 3 | 20.8 ± 2.1 | 0.5 | ||
Tacrineb | 0.19 ± 0.04 | 0.011 ± 0.001 | 17.3 |
Values are expressed as mean ± SEM.
Standard inhibitors.
Selectivity is determined as IC50 (AChE)/IC50 (BuChE).