Table 1.
MICs (Mtb) and IC50s (MurX enzyme and mammalian cells) for capuramycin (1) and its analogues, 2-4.
| Molecule | IC50 μM MurX | MIC μg/mL (MABA)a | MIC μg/mL (LORA)b |
IC50 μg/mL HepG2 cellsc |
|---|---|---|---|---|
| Capuramycin (1) | 0.127 | 12.5 | >100 | >400 |
| SQ 641 (2) | 0.098 | 1.56 | >100 | >400 |
| UT-01320 (3) | >100 | 1.50 | 2.58 | >400 |
| UT-01309 (4) | 0.095 | 2.50 | >100 | >400 |
| Rifampicin (RFP) | - | 0.20 | 1.47 | >400 |
| Isoniazid (INH) | - | 0.04-0.10 | >100 | >400 |
| Ethambutol (EMB) | - | 0.78 | >100 | >400 |
a
MABA: microplate alamar blue assay.
b
LORA: low-oxygen recovery assay.
C
Cytotoxicity against Vero monkey kidney cells was >400 μg/mL