Antibacterial activity of cystobactamids with varying E ring substitution patterns, given as minimal inhibitory concentrations (MICs) in μg mL−1, and inhibitory activity against DNA gyrase in μMe.
| ||||||||
|---|---|---|---|---|---|---|---|---|
| Compound | Y | Ring E | MIC [μg mL−1] | EC gyrase IC50 [μM] | ||||
| E. coli ΔtolCa | E. coli WTb | P. ae. ΔmexABa | P. ae. WTc | S. aureus d | ||||
| Reference 22 | CN |
|
0.06 | 0.5 | 0.25 | 2 | 0.25 | 0.08 |
| 67 | CN | –OH | ≤0.03 | >64 | >64 | >64 | >64 | 9.4 |
| 68 | NO2 |
|
≤0.03 | 1 | >64 | >64 | 64 | 0.2 |
| 69 | NO2 |
|
0.125 | 1 | 1 | >64 | 2 | nd |
| 70 | CN |
|
0.25 | >64 | >64 | >64 | >64 | nd |
| 71 | CN |
|
0.25 | >64 | >64 | >64 | >64 | nd |
| 72 | CN |
|
≤0.03 | 0.5 | >64 | >64 | 2 | nd |
| 73 | CN |
|
>64 | >64 | >64 | >64 | >64 | 0.5 |
| 74 | CN |
|
≤0.03 | 0.5 | 8 | >64 | 64 | nd |
| 75 | CN |
|
0.25 | >64 | >64 | >64 | >64 | nd |
| 76 | CN |
|
0.5 | >64 | >64 | >64 | >64 | nd |
| 77 | CN |
|
≤0.03 | >64 | >64 | >64 | >64 | 0.9 |
a
Strain provided by collaborators, see ESI.
b
DSM-1116.
c
PA14.
d
ATCC29213.
e
nd = not determined, P. ae. = P. aeruginosa.