Table 1.
Details of urease inhibition studies by conjugates of sulfa drugs with ibuprofen and flurbiprofen.
| Conjugate | IC50 (µM); Mean ± SEM (% Inhibition) |
a Vmax (app) (µM/min) |
b Km (app) (mM) |
c Ki (µM) | Mode of Inhibition |
|---|---|---|---|---|---|
| 4 | 14.26 ± 0.14 (84.2) | 3.64 | 1.66 | 8.20 | Mixed |
| 5 | 23.27 ± 0.41 (84.0) | - | - | - | - |
| 6 | 9.95 ± 0.14 (90.6) | 1.39 | 2.30 | 0.17 | Competitive |
| 7 | 50.18 ± 1.24 (71.6) | - | - | - | - |
| 8 | 12.43 ± 0.54 (87.7) | 3.0 | 0.384 | 3.01 | Mixed |
| 9 | 39.89 ± 1.17 (76.7) | - | - | - | - |
| 10 | 10.27 ± 0.11 (88.9) | 1.04 | 1.92 | 2.62 | Mixed |
| 11 | 44.46 ± 1.41 (78.7) | - | - | - | - |
| 12 | 24.92 ± 0.24 (82.1) | - | - | - | - |
| 13 | 35.30 ± 0.21 (84.6) | - | - | - | - |
| 14 | 63.42 ± 1.15 (60.4) | - | - | - | - |
| 15 | 16.74 ± 0.23 (84.1) | 1.89 | 1.80 | 7.95 | Competitive |
| 16 | 17.48 ± 0.76 (86.1) | 1.01 | 3.67 | 1.30 | Mixed |
| 17 | 13.39 ± 0.11 (86.1) | 1.56 | 5.61 | 10.40 | Competitive |
| 18 | 14.78 ± 0.16 (87.1) | 1.02 | 1.41 | 4.11 | Mixed |
| 19 | 33.83 ± 0.18 (83.8) | - | - | - | - |
| d Thiourea | 22.61 ± 0.23 (92.3) | 18.61 | 2.18 | 18.18 | Competitive |
a Vmax (app) = intercept, the maximum rate at 20 µM of inhibitor concentration. b Km (app) = slope of the line (Michaelis constant) at 20 µM of inhibitor concentration. c Ki (µM) = inhibition constant, d standard urease inhibitor.