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. 2011 Jun 7;2(8):603–607. doi: 10.1021/ml2000627

Table 1. Anti-Influenza Activities of Compounds 728.

graphic file with name ml-2011-000627_0005.jpg

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
a

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%.

b

Compound concentration to inhibit 50% of MDCK cell growth relative to control.

c

In vitro mouse liver microsome clearance calculated using the well-stirred model. See ref (15) for details.