Table 4. Anti-HCV, Metabolic, and Physical Properties Profile of Selected Analogues.

^aEC₅₀ ± SEM (n ≥ 3) is from the HCV-Luc infection assay; CC₅₀ ± SEM (n ≥ 3) is from the ATPlite cytotoxicity assay; selectivity index = CC₅₀/EC_50.

^bAll compounds were tested at 10 μM, except that compounds (S)-1, Rac-23, and Rac-29 were tested at 3.2, 3.2, and 1 μM, respectively, to avoid potential cytotoxicity.

^cAssay description: the H1HR assay addresses the H₁-histamine receptor (H1HR) inhibitory activity. The numeric value corresponds to the percentage of activation induced by histamine (250 nM) in the presence of 10 nM of compound; the HCVsc assay applies single-round infectious HCV to detect the inhibition of early stage prior to assembly in the virus replication cycle; the HCVpp assay uses an HCV pseudoparticle to determine HCVpp entry inhibition, while the murine leukemia virus pseudoparticle (MLVpp) and vesicular stomatitis virus G pseudoparticle (VSV-Gpp) were tested as controls to address viral specificity. In the HCV subgenomic replicon assay, the genotype 2a HCV replicon cell line was used to evaluate the inhibitory effect of HCV RNA replication.