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. Author manuscript; available in PMC: 2013 Jul 12.
Published in final edited form as: J Med Chem. 2012 Jun 29;55(13):6061–6075. doi: 10.1021/jm300171v

Table 5.

Summary of Antiviral and other Profiles of Compounds 31 vs 7

Compound 3l 7
Structure graphic file with name nihms388302t76.jpg graphic file with name nihms388302t77.jpg
Anti-BVDVa EC50 = 0.5 ± 0.4 μM
SI > 1000		 EC50 = 6.2 ± 4.5 μM
SI > 81
Anti-DENVb EC50 = 0.4 ± 0.2 μM
SI > 1250		 EC50 = 6.5 ± 0.6 μM
SI > 77
Solubility in PBS at pH 7.4 292 μM 315 μM
CYP3A4 inhibitionc (at 10 μM) 10.9%; - 1.9% 21.0%; 20.5%
Bioavailability (F) 92% 56%
a

tested in MDBK cells.

b

tested in BHK cells.

a&b

EC50: 50% effective concentration, measured by virus yield reduction assay; values represent average and standard deviation of results obtained from 3 independent experiments; SI: selective index, SI = CC50/EC50.

c

using midazolam and testosterone as substrates, respectively.