Table 4.
Results of the in vivo biological activity and basic bioavailability assay
| Comp | MIC50 H37Rv (μg/ml) | Results from serum Assay | Tmax (hours) | Half-life (hours)3 | Bioavailability4 | ||
|---|---|---|---|---|---|---|---|
| No serum | +10% serum | Dilution factor1 | Cmax (μg/mL) Approximate drug concentration in mouse serum2 | ||||
| INH | 0.041 | 0.12 | >1:320 | >38.4 | ND | ND | High |
| 2.HCl | 0.041 | 0.12 | 1:40–1:80 | 7.2 | 0.5 | 4.9 | Medium |
| 4a | 0.041 | 0.2 | 1:10–1:20 | 3 | ND | ND | Medium |
| 4b.HCl | 0.041 | 0.12 | 1:10–1:40 | 2.4 | 0.5 | 3.5 | Low |
| 4c.HCl | 0.014 | 0.014 | 1:80–1:160 | 2.24 | 0.5 | 1.1 | High |
| 4f.HCl | 0.014 | 0.041 | 1:40 | 1.64 | 0.5 | 1.3 | Medium |
| 4g | 0.041 | 0.2 | 1:20–1:40 | 6 | ND | ND | High |
| 4h | 0.014 | 0.041 | 1:20–1:40 | 0.82 | ND | ND | Low |
| 4k.HCl | 0.041 | 0.041 | 1:40–1:80 | 3.28 | 0.5 | 1.3 | Medium |
| 5a | 0.014 | 0.041 | 1:40 | 1.64 | ND | ND | Medium |
| 5b.HCl | 0.37 | 0.37 | 1:10–1:80 | 7.4 | 0.5 | 3.5 | Low |
1
The dilution factor represents the last dilution step of the serum samples in which drug activity was still observed in the bioassay
2
Drug levels in the mouse serum are estimated by multiplying the dilution factor by the MIC value of the drug in the presence of 10% serum;
3
Estimated based on graph of concentration vs. time curve;
4
Bioavailability factor (BF) = Cmax/MIC in presence of serum; Bioavailability: Low = BF 1–20; Medium = BF 21–80; High = BF >80 30