Table 1.
Antibacterial activity of sulfadiazine derivatives 2.
 | |||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Code | R | MIC (µM) | |||||||||||||||
| SA | MRSA | SE | EF | EC | KP | KP-E | PA | ||||||||||
| 24 h | 48 h | 24 h | 48 h | 24 h | 48 h | 24 h | 48 h | 24 h | 48 h | 24 h | 48 h | 24 h | 48 h | 24 h | 48 h | ||
| 2a | H | 500 | 500 | 250 | 250 | 62.5 | 62.5 | 31.25 | 62.5 | >500 | >500 | >500 | >500 | >500 | >500 | 500 | 500 |
| 2b | 5-F | >250 | >250 | >250 | >250 | >250 | >250 | >250 | >250 | >250 | >250 | >250 | >250 | >250 | >250 | >250 | >250 |
| 2c [4] | 5-Cl | 250 | 250 | 125 | 125 | >500 | >500 | >500 | >500 | >500 | >500 | >500 | >500 | >500 | >500 | >500 | >500 |
| 2d | 5-Br | 500 | 500 | 500 | 500 | 250 | 250 | >500 | >500 | 500 | 500 | 500 | 500 | 500 | 500 | 500 | 500 |
| 2e | 5-I | 250 | 250 | 250 | 250 | 62.5 | 125 | 250 | 500 | 250 | 250 | 500 | 500 | 500 | 500 | 500 | 500 |
| 2f | 5-NO2 | 250 | 250 | 250 | 250 | 500 | 500 | 500 | 500 | 250 | 250 | >500 | >500 | 500 | 500 | 500 | 500 |
| 2g | 5-CH3 | >250 | >250 | 125 | 125 | 125 | 125 | >250 | >250 | >250 | >250 | >250 | >250 | >250 | >250 | >250 | >250 |
| 2h | 5-CH3O | 500 | 500 | >500 | >500 | 62.5 | 62.5 | >500 | >500 | >500 | >500 | >500 | >500 | >500 | >500 | 500 | 500 |
| 2i | 5-OH | 31.25 | 31.25 | 31.25 | 31.25 | 15.62 | 15.62 | 250 | 250 | 500 | 500 | >500 | >500 | >500 | >500 | 500 | 500 |
| 2j | 5-tert-Bu | >125 | >125 | >125 | >125 | >125 | >125 | >125 | >125 | >125 | >125 | >125 | >125 | >125 | >125 | >125 | >125 |
| 2k | 6-Cl | >250 | >250 | >250 | >250 | >250 | >250 | >250 | >250 | >250 | >250 | >250 | >250 | >250 | >250 | >250 | >250 |
| 2l | 3-Cl | >500 | >500 | >500 | >500 | >500 | >500 | >500 | >500 | >500 | >500 | >500 | >500 | >500 | >500 | >500 | >500 |
| 2m | 3,5-Cl2 | 62.5 | 62.5 | 62.5 | 62.5 | 31.25 | 31.25 | >500 | >500 | >500 | >500 | >500 | >500 | 500 | 500 | >500 | >500 |
| 2n | 3-Br-5-Cl | 31.25 | 31.25 | 15.62 | 15.62 | 31.25 | 31.25 | >500 | >500 | 500 | 500 | >500 | >500 | 500 | 500 | >500 | >500 |
| 2o | 3-I-5-Cl | 15.62 | 15.62 | 15.62 | 15.62 | 31.25 | 31.25 | 250 | 250 | 250 | 250 | 500 | 500 | 500 | 500 | 500 | 500 |
| 2p | 3,5-I2 | 7.81 | 7.81 | 7.81 | 7.81 | 7.81 | 7.81 | 125 | 125 | 125 | 125 | 125 | 125 | 125 | 125 | 500 | 500 |
| 2q | - | 125 | 125 | 125 | 125 | 31.25 | 31.25 | >500 | >500 | >500 | >500 | 500 | 500 | 500 | 500 | 250 | 250 |
| SDZ 1 | - | 500 | >500 | 500 | >500 | >500 | >500 | >500 | >500 | >500 | >500 | >500 | >500 | >500 | >500 | >500 | >500 |
| BAC | - | 7.81 | 15.62 | 15.62 | 15.62 | 15.62 | 31.25 | 15.62 | 62.5 | >500 | >500 | >500 | >500 | >500 | >500 | >500 | >500 |
BAC = bacitracin; SDZ = sulfadiazine. SA: Staphylococcus aureus CCM 4516/08; MRSA: methicillin-resistant Staphylococcus aureus H 5996/08; SE: Staphylococcus epidermidis H 6966/08; EF: Enterococcus faecalis. J 14365/08. Escherichia coli CCM 4517, Klebsiella pneumoniae D 11750/08; ESBL-positive Klebsiella pneumoniae J 14368/08; PA: Pseudomonas aeruginosa CCM 1961. One or two of the best MIC value(s) for each strain are shown in bold.