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. 2018 Feb 19;8(14):7818–7831. doi: 10.1039/c7ra11872d

Structural data and inhibitory activities of compounds 1–5 against human AChE and equine BuChE.

graphic file with name c7ra11872d-u1.jpg
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
a

Values are expressed as mean ± SEM.

b

Standard inhibitors.

c

Selectivity is determined as IC50 (AChE)/IC50 (BuChE).