Table 1 In vitro urease Inhibition, anti-inflammatory, and cytotoxicity of synthetic compounds 3–27.

From: Studies on Isoniazid Derivatives through a Medicinal Chemistry Approach for the Identification of New Inhibitors of Urease and Inflammatory Markers

Compounds

R

Urease Inhibition Activity IC50 ± SEMa µM

Anti-Inflammatory Activity IC50 ± SDb µg/mL

Cytotoxicity (3T3 Cell line) IC50 ± SDb µM

3

Inactivec

Inactive

>30

4

38.8 ± 0.35

Inactive

>30

5

36.5 ± 0.14

18.5 ± 1.0

>30

6

Insoluble

Inactive

>30

7

46.3 ± 0.43

Inactive

>30

8

View full size image

44.4 ± 0.43

Inactive

>30

9

14.2 ± 1.38

26.7 ± 2.5

>30

10

15.7 ± 1.32

Inactive

>30

11

13.2 ± 1.64

Inactive

>30

12

12.3 ± 1.04

27.7 ± 2.4

>30

13

13.6 ± 1.61

Inactive

>30

14

35.8 ± 1.89

Inactive

>30

15

34.1 ± 0.45

Inactive

>30

16

21.5 ± 1.3

29.7 ± 1.7

>30

17

14.7 ± 1.01

36.9 ± 3.0

>30

18

26.3 ± 1.59

Inactive

29.5 ± 1.9

19

12.7 ± 0.8

Inactive

>30

20

22.0 ± 1.15

Inactive

>30

21

28.2 ± 1.48

Inactive

>30

22

22.1 ± 1.91

25.1 ± 0.4

>30

23

22.4 ± 1.83

12.3 ± 1.2

>30

24

63.2 ± 2.0

Inactive

>30

25

Insoluble

Inactive

>30

26

46.8 ± 1.8

25.4 ± 1.3

>30

27

Insolubled

Inactive

>30

28

Isoniazid(1)

Inactive

Inactive

28.5 ± 1.2

29

Thiourea (Standard)

21.1 ± 0.2 (Observed)

30

Aetohydaoxamic acid (standard)

20.3 ± 0.4 (Observed) 17.2 ± 0.9 (Reported)

  

31

Ibuprofen (Standard)

11.2 ± 1.9 (observed) 12.97  ±  0.23 (reported)

32

Cyclohexanamide (Standard)

0.8 ± 0.2 (observed) 0.26 ± 0.04 (reported)

  1. SEMa is the standard error of the mean, SDb is the standard deviation, and Insolubled refers to those analogue which are partially soluble in HPLC methanol used in the protocol of in vitro urease inhibition activity.
  2. Compounds showed <50% inhibition were considered as inactive.
  3. For Urease enzyme inhibition activity, screening concentration was 0.5 mM.
  4. For ROS inhibition assay screening concentration was 25 µg/mL.
  5. Note: All data were presented as mean ± standard deviation/standard error of the mean of three independent experiments where each sample was run in triplicate. The IC50 values were obtained using three concentrations of test compound, and were calculated using Excel Based Program.