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. Author manuscript; available in PMC: 2014 Jan 1.
Published in final edited form as: Bioorg Med Chem. 2012 Nov 15;21(1):102–113. doi: 10.1016/j.bmc.2012.10.058

Table 1.

Inhibition of DENV2 and WNV NS2B/NS3pro by compounds 7a-7x at 10 and 25 μM.

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Inhibitor R1 R2 DENV2 WNV
% inhibition at 10 μM % inhibition at 25 μM % inhibition at 10 μM % inhibition at 25 μM
7a H m-fluorophenyl 3.24 ± 0.93 9.11 ± 1.76 7.68 ± 0.98 10.07 ± 0.87
7b H m-chlorophenyl 5.21 ± 2.17 16.74 ± 1.97 6.15 ± 1.11 9.15 ± 0.79
7c H benzyl 3.56 ± 1.09 16.43 ± 1.84 8.27 ± 1.37 14.73 ± 1.04
7d H p-methoxybenzyl 5.27 ± 1.46 7.90 ± 1.94 5.96 ± 1.07 8.68 ± 0.95
7e methyl p-methoxybenzyl 8.08 ± 1.56 17.82 ± 1.99 4.17 ± 0.63 9.79 ± 1.02
7f benzyl benzyl 22.38 ± 0.87 31.23 ± 1.23 20.54 ± 0.91 30.12 ± 1.02
7g benzyl p-methoxybenzyl 28.49 ± 1.82 38.64 ± 1.69 24.23 ± 0.61 34.86 ± 0.45
7h benzyl m-fluorophenyl 39.03 ± 1.06 50.87 ± 1.55 30.36 ± 0.84 38.91 ± 0.61
7i benzyl m-chlorophenyl 34.27 ± 2.07 42.12 ± 1.89 29.01 ± 0.75 43.11 ± 0.71
7j benzyl p-fluorophenyl 60.34 ± 1.12 75.74 ± 1.95 51.12 ± 1.47 59.09 ± 1.35
7k benzyl p-chlorophenyl 53.25 ± 1.64 70.52 ± 2.37 53.46 ± 1.27 63.24 ± 1.24
7l benzyl p-cyanophenyl 63.86 ± 1.71 72.94 ± 1.24 63.57 ± 1.59 70.87 ± 1.32
7m benzyl phenyl 56.73 ± 0.95 69.24 ± 1.42 51.71 ± 1.16 64.09 ± 0.91
7n benzyl p-methoxyphenyl 65.49 ± 1.18 80.01 ± 1.73 68.58 ± 1.38 73.42 ± 1.22
7o benzyl p-ethoxyphenyl 40.65 ± 1.79 61.27 ± 1.71 56.09 ± 1.18 71.84 ± 2.67
7p benzyl p-pyridyl 62.43 ± 1.82 70.87 ± 1.27 63.13 ± 1.49 72.68 ± 0.88
7q benzyl m-pyridyl 58.06 ± 1.55 69.97 ± 1.02 55.83 ± 1.32 62.52 ± 0.98
7r benzyl 2-furyl 52.28 ± 1.74 64.74 ± 1.51 44.32 ± 1.53 57.67 ± 1.02
7s benzyl 2-thiophenyl 52.34 ± 2.23 69.81 ± 1.64 43.68 ± 1.36 59.66 ± 1.46
7t benzyl methyl 19.98 ± 1.45 31.59 ± 1.37 22.32 ± 0.82 40.39 ± 2.19
7u benzyl ethyl 22.54 ± 1.55 34.22 ± 2.43 25.07 ± 1.75 44.26 ± 1.69
7v benzyl propyl 25.58 ± 1.07 36.68 ± 1.91 34.94 ± 1.83 46.19 ± 2.25
7w m-fluorobenzyl m-chlorophenyl 15.97 ± 1.72 31.61 ± 2.06 27.44 ± 0.59 35.65 ± 0.22
7x phenethyl m-chlorophenyl 26.06 ± 1.15 35.01 ± 2.21 23.86 ± 0.84 33.85 ± 0.54

[WNV protease] = 28 nM; [DENV2 protease] = 25 nM *(DL) methyl, (L) benzyl, (DL) m-fluorobenzyl, (DL) phenethyl