Table 1 In vitro α-glucosidase inhibitory activity of compounds 6–22.

From: Chiral pyrimidinyl-piperazine carboxamide derivatives as potent yeast α-glucosidase inhibitors

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Cpd

Chirality

X

Y

IC50 (µM)

Cmpd

Chirality

X

Y

IC50 (µM)

6a

Racemic

3,4-Cl

4-Cl

2.41 ± 0.24a, b

13c

S

4-CF3

4-Br

1.59 ± 0.23e

6b

R

3,4-Cl

4-Cl

4.53 ± 0.21c, d

14c

S

4-CF3

4-CF3

2.63 ± 0.31a

6c

S

3,4-Cl

4-Cl

1.82 ± 0.16e

15c

S

4-CF3

2,4-Cl

12.0 ± 1.33j

7b

R

4-CF3

4-Cl

3.47 ± 0.12f

16c

S

4-CF3

3,4-Cl

1.69 ± 0.13e

7c

S

4-CF3

4-Cl

1.10 ± 0.11g

17c

S

4-CF3

3-NO2

1.03 ± 0.01g

8b

R

4-CH3

4-Cl

7.78 ± 0.15h

18c

S

4-CF3

2-OH

5.13 ± 0.49c

8c

S

4-CH3

4-Cl

2.42 ± 0.27b

19c

S

4-CF3

3-OH

2.05 ± 0.31a, b,e

9b

R

4-OCH3

4-Cl

23.41 ± 2.40i

20c

S

4-CF3

4-OH

3.71 ± 0.49f

9c

S

4-OCH3

4-Cl

7.43 ± 0.71h

21b

R

4-CF3

3-OH-4-Cl

2.08 ± 0.55a, b,e

10c

S

4-CF3

2-Cl

4.21 ± 0.25d

21c

S

4-CF3

3-OH-4-Cl

0.44 ± 0.13k

11c

S

4-CF3

3-Cl

3.45 ± 0.24f

22c

S

4-CF3

3-OBn-4-Cl

1.50 ± 0.46e, g

12c

S

4-CF3

4-F

1.82 ± 0.22e

Acarbose

-

-

-

817.38 ± 6.3l

  1. IC50 values are reported as mean ± SE. One-way ANOVA indicated significant differences among compounds (p < 0.0001). Tukey’s HSD post hoc test was used for pairwise comparisons; compounds sharing the same letter are not significantly different (p > 0.05).