Table 2. Mouse Pharmacokinetics and Physicochemical Properties of Pyrrolo- and Pyrazolopyridine Amides.
compd | 30 mg/kg po AUCa (% F) | 100 mg/kg po AUCa (% F) | CLb | Vdc | mouse PPBd | mp (°C) | sol. at pH 6.5, 7.4e |
---|---|---|---|---|---|---|---|
9 | 200 (76) | 1.9 | 0.20 | 97.9 | 243 | 1, 4 | |
10 | 49 (71) | 7.2 | 0.24 | 99.4 | 227 | <1, <1 | |
13 | 40 (100) | 15 | 0.68 | 87.1 | 173 | 80, 150 | |
14 | 52.5 | 98.4 | 220 | 1, 3 | |||
15 | 18.3 | 89.9 | 181 | 380, 740 | |||
16 | 1.09 | 90.8 | 181 | 290, 450 | |||
17 | 190 (48) | 664 (51) | 1.3 | 0.11 | 97.4 | 229 | 4, 9 |
18 | 147 (67) | 2.3 | 0.17 | 97.1 | 236 | 15, 48 | |
19 | 1080 (53) | 50.7 (1.2) | 1 | 0.11 | 99.1 | 261 | <1, 2 |
μg h/mL.
mL/min/kg.
L/kg.
Plasma protein binding (%).
μg/mL.