TABLE 1.
RNAP inhibition and antibacterial profile of selected compoundsa
| Compound | % inhibition of E. coli RNAP (at 50 μM) or IC50 value | MIC (μg/ml)b |
||||
|---|---|---|---|---|---|---|
| Gram-negative bacteria |
Gram-positive bacteria |
|||||
| E. coli TolC | E. coli K-12 | P. aeruginosa PAO1 | B. subtilis | S. aureus | ||
| CBR703 | 18 μMc | 14 | >25 | >25 | >25 | >25 |
| 7 | 35 | 9 | >25 | >25 | 23 | >25 |
| 19 | 19 μMc | 21 | >50 | >50 | 43 | >50 |
| 26 | 29 | 24 | >25 | >25 | >25 | >25 |
| 3a | n.i | 2 | >25 | >25 | 5 | 11 |
| Rifampin | 24 nMc | 6 | 7 | 13 | 5 | 0.02 |
a
No correlation between RNAP inhibition and antibacterial activities was observed, suggesting that the antibacterial activity was due to a mechanism other than RNAP inhibition. The standard deviations (SD) in these experiments were <25% (in most cases, <15%). n.i, no inhibition (<10% inhibition).
b
>25 and >50, MIC determinations were limited due to insufficient solubility of the compound.
c
IC50 value.