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. 2016 Jun 6;88(4):498–510. doi: 10.1111/cbdd.12773

Table 2.

Structure of synthetic compounds and their cholinesterase activities over acetylcholinesterase (AChE) from Electrophorus electricus and butyrylcholinesterase (BChE) from equine serum

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
a

Values are the average from three independent experiments.

b

Selectivity for AChE is defined as IC50 (BChE)/IC50 (AChE).