Table 1 Substrate scope and α-glucosidase inhibitory activity of compounds 3a–ag.

From: Design, synthesis, molecular docking, and in vitro α-glucosidase inhibitory activities of novel 3-amino-2,4-diarylbenzo[4,5]imidazo[1,2-a]pyrimidines against yeast and rat α-glucosidase

Compound

X

Ar1

Ar2

IC50 (μM)b

IC50 (μM)c

3a

H

53.8 ± 0.04

225.3 ± 43.9

3b

H

37.8 ± 0.23

150.8 ± 2.4

3c

H

85.3 ± 0.36

341.2 ± 44.2

3d

H

26.7 ± 0.28

72.9 ± 11.7

3e

H

297.0 ± 1.2

 > 600

3f.

H

193.8 ± 0.54

594.7 ± 46.8

3g

H

91.3 ± 0.4

323.2 ± 42.3

3h

H

42.6 ± 0.15

245.3 ± 50.7

3i

H

36.7 ± 0.01

180.2 ± 18.5

3j

H

114.3 ± 0.1

256.1 ± 21.2

3k

H

16.4 ± 0.36

45.0 ± 8.2

3l

H

28.0 ± 0.26

114.8 ± 13.5

3m

H

62.7 ± 0.36

332.4 ± 42.3

3n

H

48.4 ± 0.39

205.9 ± 27.4

3o

H

75.4 ± 0.42

325.8 ± 35.8

3p

H

65.4 ± 0.03

205.3 ± 37.6

3q

H

122.7 ± 0.6

404.1 ± 38.7

3r

H

128.4 ± 0.2

353.2 ± 3.9

3s

H

160.0 ± 0.36

495.3 ± 5.9

3t

H

188.5 ± 0.06

570.2 ± 70.1

3u

H

222.8 ± 0.15

 > 600

3w

H

136.0 ± 0.08

538.9 ± 3.9

3x

H

254.7 ± 0.15

 > 600

3y

Cl

78.4 ± 0.06

274.3 ± 14.9

3z

Cl

123.6 ± 0.26

461.5 ± 39.1

3aa

Cl

64.5 ± 0.15

256.1 ± 21.2

3ab

Cl

141.0 ± 1.1

431.3 ± 44.2

3ac

Cl

224.2 ± 0.15

 > 600

3ad

Cl

48.4 ± 0.39

205.9 ± 27.4

3ae

Cl

72.9 ± 0.15

292.9 ± 14.9

3af

Cl

85.4 ± 0.04

341.3 ± 44.2

3ag

Cl

102.6 ± 0.23

412.5 ± 18.4

Acarbose

–

–

–

750.0 ± 1.5

145.7 ± 9.2

  1. Values are the means of three replicates ± standard deviation (SD).
  2. bThe activity against Saccharomyces cerevisiae α-glucosidase.
  3. cThe activity against rat small intestine α-glucosidase.
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