Table 2 IC50 values and percent inhibitory activity of polysubstituted pyrroles against AChE and BChE enzymes.

From: Design, synthesis, in silico and biological evaluations of novel polysubstituted pyrroles as selective acetylcholinesterase inhibitors against Alzheimer’s disease

Compound

R1

R2

R3

AChEa

BChEa

% inhibition at 50 µM

IC50 µM

% inhibition at 50 µM

IC50 µM

4a

H

CN

4-CH3

14.71 ± 2.26

–

26.07 ± 4.09

–

4b

Methyl

CN

H

52.01 ± 4.43

37.15 ± 3.52

NA

–

4c

H

CN

H

39.75 ± 3.69

–

NA

–

4d

Methyl

COOEt

H

13.50 ± 1.58

–

13.50 ± 2.96

–

4e

Methyl

CN

4-Cl

57.05 ± 5.46

36.30 ± 4.85

18.14 ± 2.89

–

4f

H

CN

3-OCH3

33.49 ± 5.19

–

17.78 ± 2.79

–

4g

H

COOEt

H

30.78 ± 5.17

–

NA

–

4h

Methyl

CN

4-CH3

45.81 ± 2.81

67.60 ± 7.54

NA

–

4i

H

CN

4-Cl

33.94 ± 6.87

–

NA

–

4j

Methyl

COOMe

4-CH3

14.92 ± 2.45

–

28.18 ± 3.83

–

4k

Methyl

COOMe

4-Cl

13.35 ± 4.88

–

13.66 ± 2.13

–

4l

Methyl

COOEt

4-CH3

14.18 ± 2.12

–

NA

–

Donepezil

    

0.079 ± 0.05

 

10.6 ± 2.1

  1. aData represented in terms of mean ± SD.
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