Table 9.
PK Parameters of Acridone Lead Candidates in Plasma and Liver Following Single Oral Dose of 80 mg/kg Administrations in Mice
| compd | matrix |
Cmax (ng/mL) |
Tmax (h) | AUClast (ng.h/mL) |
AUCinf (ng.h/mL) |
t1/2 (h) |
CL/F (mL/h/kg) |
Vz/F (mL/kg) |
MRT b (h) |
|---|---|---|---|---|---|---|---|---|---|
| 26 (T111) | plasma | 17.2 | 0.50 | 392 | 508 | 23.6 | 157510 | 5370641 | 17.6 |
| liver | 1732 | 7.0 | 46232 | 57122 | 14.0 | 1697 | 34167 | 19.9 | |
| 87 (T121) | plasma | 42.0 | 2.0 | 105 | 518 | 8.70 | 154543 | 1940321 | 7.20 |
| liver | 1193 | 4.0 | 20416 | 20494 | 6.00 | 3903 | 33802 | 10.0 | |
| 90 (T122) | plasma | 21.5 | 1.0 | 225 | 236 | 4.90 | 339065 | 2402651 | 10.18 |
| liver | 1967 | 0.50 | 19188 | 19271 | 6.10 | 4151 | 36779 | 7.60 | |
| 91 (T124) | plasma | 19.5 | 1.0 | 175 | 187 | 5.90 | 428286 | 3648089 | 6.20 |
| liver | 925 | 1.0 | 11485 | 11570 | 6.80 | 6914 | 67596 | 8.30 | |
| 107 (T129) | plasma | 170 | 0.5 | 1680 | 1705 | 4.30 | 46906 | 290091 | 5.70 |
| liver | 684 | 2.0 | 8547 | 8674 | 4.00 | 9223 | 53720 | 5.80 | |
| Primaquine | plasma | 531 | 0.50 | 1256 | 1314 | 1.84 | 16415 | 43801 | 2.30 |
| liver | 8148 | 0.50 | 27450 | 27665 | 4.27 | 724 | 4418 | 4.50 |
Cmax: maximum plasma or hepatic concentration; Tmax: time to Cmax; AUXlast: area under the concentration-time curve from 0 up to the last sampling time at which a quantifiable concentration is found; AUCinf: area under the concentration-time curve from 0 up to infinity; t1/2: apparent elimination half-life; CL/F: apparent oral clearance; Vz/F: apparent volume of distribution after oral dose; MRT b: mean residence time, body.