Table 2.
Antimycobacterial activity of sulfadiazine derivatives 2.
| Code | R | MIC (µM) | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Mtb. 331/88 | M. avium 330/88 | M. kansasii 235/80 | M. kansasii 6509/96 | ClogP | ||||||||
| 14 d | 21 d | 14 d | 21 d | 7 d | 14 d | 21 d | 7 d | 14 d | 21 d | |||
| 2a | H | 16 | 32 | 125 | 250 | 8 | 16 | 32 | 8 | 16 | 32 | 2.5 |
| 2b | 5-F | 125 | 125 | 500 | 1000 | 62.5 | 125 | 250 | 125 | 250 | 250 | 2.65 |
| 2c [4] | 5-Cl | 125 | 250 | 125 | 125 | 8 | 16 | 32 | 16 | 32 | 32 | 3.05 |
| 2d | 5-Br | 16 | 32 | 125 | 125 | 32 | 62.5 | 62.5 | 32 | 32 | 62.5 | 3.32 |
| 2e | 5-I | 62.5 | 125 | 125 | 250 | 32 | 62.5 | 125 | 32 | 32 | 62.5 | 3.85 |
| 2f | 5-NO2 | 250 | 250 | 500 | 1000 | 125 | 250 | 500 | 125 | 250 | 250 | 2.15 |
| 2g | 5-CH3 | 125 | 125 | 500 | 1000 | 125 | 125 | 250 | 62.5 | 62.5 | 125 | 2.98 |
| 2h | 5-CH3O | 32 | 62.5 | 125 | 125 | 16 | 32 | 62.5 | 16 | 16 | 32 | 2.37 |
| 2i | 5-OH | 125 | 125 | 500 | 1000 | 62.5 | 125 | 125 | 62.5 | 125 | 125 | 2.11 |
| 2j | 5-tert-Bu | 32 | 62.5 | 125 | 125 | 16 | 32 | 62.5 | 16 | 16 | 32 | 4.2 |
| 2k | 6-Cl | 125 | 125 | 250 | 250 | 62.5 | 125 | 250 | 62.5 | 125 | 125 | 3.05 |
| 2l | 3-Cl | 32 | 62.5 | 125 | 250 | 16 | 32 | 62.5 | 16 | 16 | 32 | 3.05 |
| 2m | 3,5-Cl2 | 125 | 125 | 250 | 500 | 125 | 250 | 500 | 62.5 | 125 | 250 | 3.61 |
| 2n | 3-Br-5-Cl | 125 | 125 | 250 | 500 | 125 | 125 | 250 | 62.5 | 125 | 125 | 3.88 |
| 2o | 3-I-5-Cl | 125 | 125 | 500 | 500 | 125 | 250 | 250 | 62.5 | 125 | 125 | 4.41 |
| 2p | 3,5-I2 | 250 | 250 | 250 | 500 | 125 | 250 | 250 | 62.5 | 125 | 250 | 5.21 |
| 2q | - | 125 | 125 | 500 | 500 | 125 | 250 | 250 | 62.5 | 62.5 | 125 | ND |
| SDZ 1 | - | 32 | 62.5 | 62.5 | 62.5 | 16 | 16 | 32 | 8 | 8 | 8 | 0.21 |
| INH | - | 0.5 | 1 | >250 | >250 | >250 | >250 | >250 | 8 | 8 | 8 | - |
INH = isoniazid; SDZ = sulfadiazine. Mtb. = Mycobacterium tuberculosis. ND = not determined. One or two of the best MIC value(s) for each strain are shown in bold.