Table 2. MraY Inhibitory and Anti-Pseudomonas Activity of Analogues 21–29.
| MIC (μg/mL)a |
||||||
|---|---|---|---|---|---|---|
| compound | MraY IC50 (nM) | P. aeruginosa PAOl | P. aeruginosa YY165 (ΔmexB) | P. aeruginosa ATCC 25619 | P. aeruginosa SR 27156 | P. aeruginosa ATCC 27853 |
| 21 | 1491 | >64 | >64 | >64 | >64 | >64 |
| 22 | 97.3 | >64 | >64 | >64 | >64 | >64 |
| 23 | 225 | >64 | >64 | >64 | >64 | >64 |
| 24 | 9.8 | >64 | >64 | 32 | >64 | >64 |
| 25 | 2.1 | 32 | 16 | 16 | 16 | 32 |
| 26 | 1.6 | 16 | 8 | 16 | 16 | 32 |
| 27 | 0.14 | 16 | 8 | 8 | 8 | 16 |
| 28 | 12.2 | 32 | 16 | 16 | 16 | 16 |
| 29 | 0.60 | 4 | 4 | 8 | 8 | 8 |
| 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.