Table 2.
Sulfonamide inhibitors of mycobacterial Lpd.
| ID | Structure | Ki (Lpd), nM | Ki (PDH), nM | SI* |
|---|---|---|---|---|
| SL932 |
|
37±5 | 78±6 | >2700 |
| SL809 |
|
93±12 | 155±12 | >1075 |
| SL827 |
|
140±9 | 155±14 | >714 |
| SL917 |
|
233±15 | 289±9 | >429 |
| SL418 |
|
143±12 | 333±28 | 1300 |
*
Due to the solubility limit of the compounds the highest concentration tested was 100 μM. No inhibition of hLpd by SL932, SL809, SL827 and SL917 was observed at 100 μM and the SI values were calculated using 100 μM as a substitute Ki for hLpd. The resulting SI therefore reflects the lower limit of the SI value and in fact will be much greater, which is indicated by the > symbol.