Table 2. Anti-Influenza Activities of Sulfonamide Analogues and Their DMPK Profiles.
compd | R | EC50 (CPE, μM) a | CC50 (μM) b | IC50 (μM) c | HLM CLh (mL/min/kg) d | MLM CLh (mL/min/kg) b |
---|---|---|---|---|---|---|
31 | 3-F | 0.089 | 55.0 | 0.58 | 7.2 | 42.3 |
32 | 3-Cl | 0.044 | 8.4 | 0.23 | 12.1 | 51.8 |
33 | 3-CF3 | 1.36 | 19.5 | 2.91 | 5.1 | 39.6 |
34 | 2-Me | 0.56 | 81.5 | 1.13 | 8.5 | 43.7 |
35 | 2-OMe | 2.62 | >100 | 4.16 | 10.0 | 66.4 |
40 | 2-Cl | 0.086 | 71.2 | 0.25 | 8.4 | 42.5 |
Compound concentration to inhibit the cytopathic effect based on OD measurement. Values are means of three determinations run in duplicate, SD ± 15%.
See the notes in Table 1.
Half maximal inhibition concentration to prevent hemolysis of chicken RBCs; values are the average of two duplicate experiments, SD ± 20%.
In vitro human liver microsome clearance calculated using the well-stirred model.