Table 1. Antimicrobial activity of Debio-1452 and derivatives.
The aqueous solubility limit of Debio-1452 prevents determining actual MIC values that are above 32 μg/mL. MIC values were determined using the micro-dilution broth method as outlined by the Clinical and Laboratory Standards Institute (http://clsi.org/) (CLSI. Methods for Dilution Antimicrobial Susceptibility Tests for Bacteria That Grow Aerobically. 11th ed. CLSI standard M07. Wayne, PA: Clinical and Laboratory Standards Institute; 2018). All experiments were performed in biological triplicate.
| Bacterial Strain | MIC (μg/mL) | ||
|---|---|---|---|
| Debio-1452 | Debio-1452-NH3 | 8 | |
| WT Gram-positive | |||
| S. aureus ATCC29213 | 0.008 | 0.03 | 0.016 |
| Gram-negative permeability mutant | |||
| E. coli ΔtolC JW5503 | 0.031 | 0.062 | 0.125 |
| E. coli ΔrfaC JW3596 | 0.5 | 0.25 | 0.25 |
| WT Gram-negative | |||
| E. coli MG1655 | >32 | 4 | >32 |
| E. coli BAA-2340 | >32 | 4 | >32 |
| E. coli AR-0493 | >32 | 4 | >32 |
| E. cloacae ATCC 29893 | >32 | 8 | >32 |
| K. pneumoniae BAA-1705 | >32 | 8 | >32 |
| K. pneumoniae S47889 | >32 | 8 | >32 |
| A. baumannii W41979 | >32 | 4 | >32 |
| A. baumannii F19521 | >32 | 4 | >32 |
| P. aeruginosa PA01 | >32 | >64 | >32 |