Table 1. Anti-Influenza Activities of Compounds 7–28.
compd ID | Ar | R | EC50 (CPE, μM) a | CC50 (μM) b | MLM CLh (mL/min/kg) c |
---|---|---|---|---|---|
1 | salicylamide | H | 0.030 | >50 | 76.7 |
7 | 1H-indazol-3-yl | H | 6.90 | >100 | 45.2 |
8 | quinazolin-2-yl | H | 8.5 | 26.7 | 82.9 |
9 | benzothiazol-2-yl | H | 2.12 | 36.8 | 85.4 |
10 | benzothiazol-2-yl | 6-F | 2.5 | 16.2 | 78.2 |
11 | benzothiazol-2-yl | 6-Cl | >50 | 4.2 | |
12 | pyridin-2-yl | H | 4.43 | >100 | 80.6 |
13 | pyridin-2-yl | 5-CF3 | 3.39 | 30.5 | |
14 | pyridin-2-yl | 6-CF3 | 0.22 | 13.5 | 82.3 |
15 | Ph | H | 0.43 | 37 | 85.6 |
16 | Ph | 2-Cl | 0.52 | 6.9 | |
17 | Ph | 3-Cl | 0.057 | 9.7 | 86.1 |
18 | Ph | 4-Cl | 0.44 | 8.1 | |
19 | Ph | 2-CF3 | 0.15 | 6.6 | |
20 | Ph | 3-CF3 | 0.042 | 7.8 | 83.8 |
21 | Ph | 3-CF3, 5-Cl | 0.044 | 6.7 | 49.8 |
22 | Ph | 3-Cl, 5-F | 0.015 | 4.4 | 85.1 |
23 | Ph | 3-CF3, 4-Cl | 0.018 | 2.8 | 62.4 |
24 | Ph | 3-CN | 0.25 | 46.9 | 84 |
25 | Ph | 3-PhO | >100 | 6.0 | |
26 | Ph | 3-CONH2 | 37.9 | >100 | 43.0 |
27 | Ph | 3-SO2Me | 0.93 | >50 | 65.3 |
28 | Ph | 3-SO2NH2 | 0.21 | >100 | 37.2 |
Compound concentration to inhibit 50% of the cytopathic effect based on OD measurement. Values are the average of ≥two determinations run in duplicate, SD ± 15%.
Compound concentration to inhibit 50% of MDCK cell growth relative to control.
In vitro mouse liver microsome clearance calculated using the well-stirred model. See ref (15) for details.