Table 1.

The Structure, In Vitro Anti-Hepatitis C Virus (HCV) Activity, and ADME Properties of Current Lead Compounds in the Chlorcyclizine (CCZ) Series

^a Me, methyl; Et, ethyl; ⁿPr, ⁿpropyl; ⁱPr, isopropyl.

^b 50% viral inhibition (EC₅₀) ± standard error of the mean (SEM) (n ≥ 3) from the HCV-Luc infection assay.

^c 50% cytotoxicity (CC₅₀) from the ATPlite cytotoxicity assay.

^d Selectivity index = CC₅₀ (Huh-7.5.1) /EC₅₀.

^e Residual H₁ histamine receptor activity (H₁HR) expressed as % of dimethyl sulfoxide (DMSO) negative control at 10 nM concentration. H₁HR activity of racemic CCZ at 10 nM, of 16% DMSO control.

Abbreviations: ADME, absorption, distribution, metabolism, and excretion; Cmpd, compound; PHH, primary human hepatocytes; ND, not determined.