1393355-16-2Relevant academic research and scientific papers
C-6 aryl substituted 4-quinolone-3-carboxylic acids as inhibitors of hepatitis C virus
Chen, Yue-Lei,Zacharias, Jeana,Vince, Robert,Geraghty, Robert J.,Wang, Zhengqiang
, p. 4790 - 4800 (2012)
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.
