Table 4.
Pharmacokinetic properties, inhibitory activity, and physicochemical properties
| Linezolid | 19a | 19b | |
|---|---|---|---|
| Aq. Solubility (μg/mL) | >67.47 | >52.15 | >48.49 |
| Stability at gastric pH (% remaining 24 h) | 98% | 94% | 89% |
| t1/2 microsomes (min)a | >216.8 | 170.0 | 128.3 |
| Cytotoxicity EC50 (μM)b | >30 | > 30 | >30 |
| CYP inhibition (μM)c | >100 | > 100 | >100 |
| Mt protein synthesis inhibition IC50 (μM)d | 8.19 | 30 | >30 |
a
Metabolic stability performed with mouse liver microsomes
b
Cytotoxicity against HepG2 cells using CellTiter Glo
c
Measured against CYP1A2, 2C9, 2C19, 2D6, 3A4
d
MitoBiogenesis In-Cell ELISA assay for COXI and SDH-A mitochondrial proteins