Article
Discovery of benzophosphadiazine drug candidate IDX375: A novel hepatitis C allosteric NS5B RdRp inhibitor.
Bioorganic & medicinal chemistry letters - 1 Jun 2017
Paparin Jean-Laurent, Amador Agnès, Badaroux Eric, Bot Stéphanie, Caillet Catherine, Convard Thierry, Da Costa Daniel, Dukhan David, Griffe Ludovic, Griffon Jean-François, LaColla Massimiliano, Leroy Frédéric, Liuzzi Michel, Giulia Loi Anna, McCarville Joe, Mascia Valeria, Milhau Julien, Onidi Loredana, Pierra Claire, Rahali Rachid, Rosinosky Elodie, Sais Efisio, Seifer Maria, Surleraux Dominique, Standring David, Dousson Cyril B
Abstract excerpt
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 paper describes the discovery of a novel family of HCV NS5B non-nucleoside inhibitors inspired by the bioisosterism between sulfonamide and phosphonamide. Systematic structural...
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