Table 1.
In vitro anti-tuberculosis activity of nNF derivatives (nNF-C1–nNF-C20) against actively replicating M. tuberculosis H37Rv
| MIC90 REPLICATING M. tuberculosis | ||||
|---|---|---|---|---|
| Compound | μg/ml (range) | μg/ml (median) | μM (median) | |
| High activity | nNF-C1 | 0.062–0.25 | 0.125 | 0.42 |
| nNF-C2 | 0.062–0.125 | 0.062 | 0.21 | |
| nNF-C3 | 0.25–0.5 | 0.5 | 1.68 | |
| nNF-C4 | 0.03–0.125 | 0.125 | 0.46 | |
| nNF-C5 | 0.25–0.5 | 0.25 | 1.05 | |
| nNF-C6 | 0.5 | 0.5 | 1.63 | |
| nNF-C8 | 0.062–0.25 | 0.125 | 0.46 | |
| nNF-C16 | 0.03–0.062 | 0.062 | 0.25 | |
| nNF-C18 | 0.125–0.25 | 0.25 | 0.78 | |
| nNF-C20 | 0.125 | 0.125 | 0.4 | |
| Moderate activity | nNF-C7 | 4–8 | 4 | 15.55 |
| nNF-C11 | 8–16 | 8 | 32.89 | |
| nNF-C12 | 2–8 | 4 | 14.85 | |
| nNF-C14 | 0.5–4 | 2 | 8.8 | |
| nNF-C17 | 2–4 | 2 | 8.29 | |
| Low/No activity | nNF-C9 | >32 | >50 | |
| nNF-C10 | >32 | >100 | ||
| nNF-C13 | >32 | >100 | ||
| nNF-C15 | 32 | >100 | ||
| nNF-C19 | 16 | >50 | ||
| TB antibiotics | INH | 0.01–0.04 | 0.03 | 0.218 |
| RIF | 0.062–0.125 | 0.125 | 0.35 | |
| PA-284 | 0.25–0.5 | 0.25 | 0.31 | |
MIC90 determination was carried out by REMA. According to their activity against replicating bacteria, nNF compounds were divided in three different groups: High activity (MIC ≤ 0.5 μg/ml), Moderate Activity (MIC ≤ 8 μg/ml) and No Activity (MIC ≥ 16 μg/ml). MIC90 values are expressed in μg/ml (range and median) and μM (median).