Table 2.
Mycobacterial enzyme activity inhibition results.
| Comp. code | R1 | R2 | % inhibition at 50 μM against L-MtAlaDH | L-MtAlaDH IC50 (μM) |
% inhibition at 50 μM against MtLAT | % inhibition at 50 μM against MtCM | % inhibition at 50 μM against MtPS |
|---|---|---|---|---|---|---|---|
| 1a | 4-Br | 3-F | 69.94 | 39.75 | 7.80 | 40.50 | 7.47 |
| 1b | 4-Br | 3-Cl | 59.46 | 41.12 | 18.73 | 43.50 | 3.89 |
| 1c | 4-Br | 4-Cl | 39.35 | >50 | 29.10 | 48.31 | 13.25 |
| 1d | 4-Br | 3,4-di-Cl | 59.02 | 31.92 | 30.27 | 41.30 | 20.54 |
| 1e | 4-Br | 3-CF3 | 42.08 | >50 | 40.20 | 53.20 | 17.76 |
| 1f | 4-Br | 4-CF3 | 69.28 | 34.73 | 26.15 | 52.09 | 11.33 |
| 1g | 4-Br | 3-Br | 22.62 | >50 | 12.42 | 46.07 | 18.76 |
| 1h | 4-Br | 4-Br | 34.35 | >50 | 18.25 | 38.19 | 18.33 |
| 1i | 4-Br | 4-F | 54.58 | 15.58 | 2.90 | 46.67 | 5.41 |
| 1j | 4-Cl | 3-Cl | 12.30 | >50 | 29.30 | 54.56 | 3.64 |
| 1k | 4-Cl | 4-Cl | 18.73 | >50 | 38.00 | 43.78 | 14.74 |
| 1l | 4-Cl | 3-F | 61.87 | 23.11 | 8.06 | 50.75 | 17.93 |
| 1m | 4-Cl | 4-F | 57.70 | 42.26 | 20.12 | 49.33 | 7.76 |
| 1n | 4-Cl | 4-Br | 70.64 | 29.17 | 17.29 | 50.19 | 6.57 |
| 1o | 4-Cl | 3,4-di-Cl | 44.46 | >50 | 18.24 | 60.96 | 23.01 |
| 1p | 4-Cl | 3-Br | 54.64 | 36.11 | 19.13 | 37.41 | 20.59 |
| 1q | 4-Cl | 3-CF3 | 73.88 | 36.32 | 19.05 | 50.02 | 11.53 |
| 1r | 4-Cl | 4-CF3 | 47.28 | >50 | 23.18 | 50.05 | 26.25 |
| 1s | 5-Cl | 3-Cl | 73.94 | 4.96 | 53.64 | 60.12 | 11.18 |
| 1t | 5-Cl | 3-Br | 41.51 | >50 | 12.86 | 57.58 | 5.04 |
| 1u | 5-Cl | 3-F | 59.85 | 39.20 | 23.42 | 52.36 | 22.22 |
| 1v | 5-Cl | 4-F | 69.07 | 34.47 | 37.29 | 52.05 | 17.28 |
| 1w | 5-Cl | 4-Br | 14.97 | >50 | 40.28 | 52.84 | 14.51 |
| 1x | 5-Cl | 4-Cl | 58.62 | 46.51 | 20.18 | 53.79 | 11.17 |
| 1y | 5-Cl | 3,4-di-Cl | 26.30 | >50 | 28.17 | 56.65 | 12.38 |
| 1z | 5-Cl | 3-CF3 | 58.32 | 17.82 | 10.01 | 43.49 | 4.51 |
| 1zz | 5-Cl | 4-CF3 | 64.82 | 37.49 | 19.83 | 54.09 | 8.26 |
The best results for each enzyme are shown in bold.