Table 3. In vivo pharmacokinetic parameters in lungs for bicyclic 4-nitroimidazole analogs.
Compound | Dose(mg/kg) | Lung PK parameters | Lung to Plasma ratio | ||||
Cmax (µg/g) | AUC24 (µg.h/g) | Tmax (hr) | T1/2 (p.o.) | Cmax | AUC24 | ||
PA-824 | 25 | 17.8 | 139.9 | 0.3 | 4.8 | 3.0 | 2.7 |
NI-622 | 50 | 10.2 | 71.1 | 0.5 | 1.8 | 0.7 | 0.7 |
NI-644 | 50 | 7.5 | 38.1 | 1 | 2.9 | 0.5 | 0.4 |
Amino-824 | 10 | 1.4 | 4.5 | 0.5 | 1.3 | 0.8 | 0.8 |
AminoEthyl-824 | 10 | 1.6 | 5.2 | 0.5 | 1.2 | 1.6 | 1.8 |
NI-135 | 25 | 5.5 | 18.6 | 0.5 | 3.3 | 4.6 | 3.9 |
NI-147 | 25 | 0.5 | 2.6 | 0.1 | - | - | - |
NI-136 | 25 | 7.2 | 39.8 | 0.5 | 2.5 | 3.6 | 3.7 |
NI-176 | 25 | 4.8 | 30.3 | 0.5 | 4.3 | 2.2 | 2.2 |
NI-269 | 25 | 5.4 | 27.5 | 0.3 | 2.7 | 1.9 | 1.7 |
NI-182 | 25 | 11.4 | 73.2 | 0.5 | 1.9 | 3.3 | 3.3 |
NI-145 | 25 | 4.2 | 34.6 | 2 | 4.1 | 2.3 | 2.1 |
NI-297 | 25 | 16.3 | 233.4 | 8 | 4.6 | 2.7 | 2.4 |
NI-302 | 25 | 9.7 | 100.3 | 2 | 4.1 | 0.8 | 0.7 |