Table 1. Screening of Muraymycin Analogues 1–19 as Anti-Pseudomonas Agents.
| MIC (μg/mL)a |
||||||
|---|---|---|---|---|---|---|
| compound | MraY IC50 (nM) | P. aeruginosa PAO1 | P. aeruginosa YY165 (ΔmexB) | P. aeruginosa ATCC 25619 | P. aeruginosa SR 27156 | P. aeruginosa ATCC 27853 |
| 1 | 2.8 | >64 | 64 | 64 | 32 | >64 |
| 2 | 1.1 | >64 | >64 | >64 | >64 | >64 |
| 3 | 0.8 | >64 | >64 | >64 | >64 | >64 |
| 4 | 0.7 | >64 | >64 | >64 | >64 | >64 |
| 5 | 0.8 | >64 | >64 | >64 | >64 | >64 |
| 6 | 4.2 | >64 | >64 | >64 | >64 | >64 |
| 7 | 2.4 | >64 | 32 | 64 | 64 | >64 |
| 8 | 3.8 | 64 | 32 | 32 | 32 | 64 |
| 9 | 2.2 | 16 | 8 | 8 | 16 | 32 |
| 10 | 8.5 | >64 | 16 | 16 | 64 | 64 |
| 11 | 2.6 | >64 | 32 | 32 | >64 | >64 |
| 12 | 2.7 | 64 | 32 | 32 | 64 | >64 |
| 13 | 29.6 | >64 | >64 | >64 | >64 | >64 |
| 14 | 6.4 | >64 | >64 | 64 | >64 | >64 |
| 15 | 9.6 | >64 | >64 | 64 | >64 | >64 |
| 16 | 8.1 | >64 | >64 | 64 | >64 | >64 |
| 17 | 13.5 | >64 | 64 | 64 | >64 | >64 |
| 18 | 33.1 | >64 | >64 | 64 | >64 | >64 |
| 19 | 105 | >64 | >64 | >64 | >64 | >64 |
| doripenem | n.d. | 0.5 | 0.25 | 0.063 | 0.031 | 0.5 |
a
MICs were determined by a microdilution broth method as recommended by the CLSI with cation-adjusted Mueller–Hinton broth (CA-MHB). Serial 2-fold dilutions of each compound were made in appropriate broth, and the plates were inoculated with 5 × 104 CFU of each strain in a volume of 0.1 mL. Plates were incubated at 35 °C for 20 h, and then MICs were scored.