Table 5. PK Parameters in Mouse of Substituted Benzothiazoles 12 and 16.
| PK parameters after single 10 mg/kg IV dose | compound 12 | compound 16 | |
|---|---|---|---|
| plasma | C0 (μg/mL)a | 92.2 | 175.7 |
| AUClast (μg*h/mL)b | 610.4 | 517.1 | |
| CL (mL/min/kg)c | 0.3 | 0.3 | |
| t1/2 (h)d | 6.2 | 6.5 | |
| ELFe | C0 (μg/mL) | 2.7 | 2.7 |
| AUClast (μg*h/mL) | 57.7 | 27.0 | |
| CL (mL/min/kg) | 1.5 | 5.2 | |
| t1/2 (h) | 25.8 | 9.5 | |
| lung penetration (AUClast plasma/AUClast ELF) | 9.54% | 5.22% | |
a
Concentration at time zero.
b
Area under the curve between first and last measurement.
c
Clearance.
d
Half-life.
e
Epithelial lining fluid; concentrations determined by normalizing bronchoalveolar lavage fluid (BALF) concentrations to plasma urea concentrations to adjust for dilution during the sampling procedure.