Table 1.
Inhibitory effect of the NPT and BPT compounds on the Rpf-mediated hydrolysis of mycobacterial peptidoglycan and on bacterial growth
| № | Chemical name | Formula | IC50 Rpf-hydrolysis of PG, µM | MIC of the compound, µM | ||
|---|---|---|---|---|---|---|
| M. smegmatis | M. tuberculosis | M. luteus | M. smegmatis | |||
| (I) | 4-Benzoyl-2-nitrophenyl thiocyanate |
|
2.4 ± 0.7 | 4.0 ± 2.1 | 25–35 | 18–35 |
| (II) | 3-Benzoylphenyl thiocyanate |
|
0.4 ± 0.0 | 1.7 ± 0.4 | 32–42 | 32–42 |
| (III) | 4-Benzoylphenyl thiocyanate |
|
0.9 ± 0.5 | 1.2 ± 0.5 | 25–32 | 21–42 |
| (IV) | Bis(4-thiocyano-3-nitrophenyl)methanone |
|
3.7 ± 0.2 | 5.8 ± 2.0 | 47–52 | 26–52 |
| (V) | Bis(4-thiocyanophenyl)methanone |
|
2.5 ± 0.6 | 4.3 ± 2.4 | 48–51 | 34 |
| (VI) | Bis(3-thiocyanophenyl)methanone |
|
2.0 ± 0.8 | 3.6 ± 1.2 | 34–41 | 34 |
Enzymatic activity was calculated as a value of the half maximal inhibitory concentration (IC50). IC50 values were calculated in the enzymatic assay of the Rpf-mediated PG hydrolysis (concentration of RpfB280–326 was 10 μg/ml). The experiment was repeated three times with nearly identical results (mean values ± SD are shown)
MIC was evaluated as the minimal inhibitory concentration of the compounds sufficient for suppression of active growth of the bacteria. The experiments were repeated at least three times with nearly identical results (mean values ± SD are shown)