Table 1. Inhibitory Activity of Compounds 9 and 10 against MurD and MurE Ligases and Their Antibacterial Activity.
IC50 (μM) |
MIC (μg/mL) |
|||||
---|---|---|---|---|---|---|
enzyme | I | 9 | 10 | bacterial strain | 9 | 10 |
E. coli MurD ligase | 35 | 8.2 ± 0.6 | 36 ± 5 | S. aureus ATCC 29213 | 8 | >128 |
S. aureus MurD ligase | ND | 6.4 ± 1.0 | 100 ± 5 | MRSA ATCC 43300 | 8 | >128 |
E. coli MurE ligase | 64%a | 180 ± 60 | ∼200b | E. faecalis ATCC 29212 | 64 | >128 |
S. aureus MurE ligase | ND | 17 ± 1.5 | >200c | E. coli ATCC 25922 | >128 | >128 |
P. aeruginosa ATCC 27853 | >128 | >128 |
Residual activity (RA) at 500 μM compound.
Residual activity at 200 μM compound: 51 ± 2%.
No inhibitory activity at 200 μM compound; ND, not determined.