Table 1.
Representative derivatives of SFN with their corresponding antibacterial activities (MIC against S. aureus NCTC 8325), shift of activity in the presence of menaquinone-4 (MK-4; 100 μg/mL), and SpsB activation potential. Data are derived from three biologically independent experiments performed in triplicates and SpsB activity is given as mean value ± SD. A full list of compounds and corresponding activities can be found in Supplementary Data 1 and MIC shifts of PK150, SFN and 1-164 at different concentrations of MK-4 are listed in Supplementary Data 2.
| MIC (μM) |
MIC at 100 μg/mL MK-4 (μM) |
SpsB activity (normalized) at 50 μM |
||
|---|---|---|---|---|
| SFN |  |
3 | 20 | 1.64 ± 0.12 |
| 1-134 |  |
> 100 | n.a. | 1.12 ± 0.08 |
| 1-163 |  |
> 100 | n.a. | 1.33 ± 0.20 |
| SFN-C |  |
> 100 | n.a. | 1.18 ± 0.16 |
| 3-001 |  |
10 | 30 | 1.58 ± 0.28 |
| 2-013 |  |
3 | 7 | 1.91 ± 0.25 |
| 3-004 |  |
3 | >100 | 1.49 ± 0.16 |
| 3-005 |  |
0.6 | 3-5 | 2.12 ± 0.25 |
| 3-006 |  |
0.5 | 5 | 2.10 ± 0.14 |
| PK150 |  |
0.3 | 1-3 | 2.54 ± 0.39 |
| PK150-C |  |
> 100 | n.a. | 1.15 ± 0.01 |
| 1-159 |  |
10 | >100 | 1.40 ± 0.01 |
| 1-160 |  |
30 | 50 | 1.64 ± 0.16 |
| 1-164 |  |
0.5 | 3 | 1.42 ± 0.08 |