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  • Title: C-6 aryl substituted 4-quinolone-3-carboxylic acids as inhibitors of hepatitis C virus.
    Author: Chen YL, Zacharias J, Vince R, Geraghty RJ, Wang Z.
    Journal: Bioorg Med Chem; 2012 Aug 01; 20(15):4790-800. PubMed ID: 22748708.
    Abstract:
    Quinolone-3-carboxylic acid represents a highly privileged chemotype in medicinal chemistry and has been extensively explored as antibiotics and antivirals targeting human immunodeficiency virus (HIV) integrase (IN). Herein we describe the synthesis and anti-hepatitis C virus (HCV) profile of a series of C-6 aryl substituted 4-quinlone-3-carboxylic acid analogues. Significant inhibition was observed with a few analogues at low micromolar range against HCV replicon in cell culture and a reduction in replicon RNA was confirmed through an RT-qPCR assay. Interestingly, evaluation of analogues as inhibitors of NS5B in a biochemical assay yielded only modest inhibitory activities, suggesting that a different mechanism of action could operate in cell culture.
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