Article
Synthesis of potent and broad genotypically active NS5B HCV non-nucleoside inhibitors binding to the thumb domain allosteric site 2 of the viral polymerase.
Bioorganic & medicinal chemistry letters - 15 Sept 2016
Pierra Rouvière Claire, Amador Agnès, Badaroux Eric, Convard Thierry, Da Costa Daniel, Dukhan David, Griffe Ludovic, Griffon Jean-François, LaColla Massimiliano, Leroy Frédéric, Liuzzi Michel, Loi Anna Giulia, McCarville Joe, Mascia Valeria, Milhau Julien, Onidi Loredana, Paparin Jean-Laurent, Rahali Rachid, Sais Efisio, Seifer Maria, Surleraux Dominique, Standring David, Dousson Cyril
Abstract excerpt
The hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase (RdRp) plays a central role in virus replication. NS5B has no functional equivalent in mammalian cells and, as a consequence, is an attractive target for selective inhibition. This Letter describes the discovery of a new family of HCV NS5B non-nucleoside inhibitors, based on the bioisosterism between amide and phosphonamidate functions. As part of this...
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