Allosteric inhibition of the hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase enzyme has recently emerged as a viable strategy toward blocking replication of viral RNA in cell-based systems. We report here a novel class of allosteric inhibitor of NS5B that shows potent affinity for the NS5B enzyme and effective inhibition of subgenomic HCV RNA replication in HUH-7 cells. Inhibitors from this class have promising characteristics for further development as anti-HCV agents.
Development and preliminary optimization of indole-N-acetamide inhibitors of hepatitis C virus NS5B polymerase / S. Harper, B. Pacini, S. Avolio, M. Di Filippo, G. Migliaccio, R. Laufer, R. De Francesco, M. Rowley, F. Narjes. - In: JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0022-2623. - 48:5(2005), pp. 1314-1317.
Development and preliminary optimization of indole-N-acetamide inhibitors of hepatitis C virus NS5B polymerase
R. De Francesco;
2005
Abstract
Allosteric inhibition of the hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase enzyme has recently emerged as a viable strategy toward blocking replication of viral RNA in cell-based systems. We report here a novel class of allosteric inhibitor of NS5B that shows potent affinity for the NS5B enzyme and effective inhibition of subgenomic HCV RNA replication in HUH-7 cells. Inhibitors from this class have promising characteristics for further development as anti-HCV agents.
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