1126651-91-9Relevant academic research and scientific papers
Discovery of benzophosphadiazine drug candidate IDX375: A novel hepatitis C allosteric NS5B RdRp inhibitor
Paparin, Jean-Laurent,Amador, Agnès,Badaroux, Eric,Bot, Stéphanie,Caillet, Catherine,Convard, Thierry,Da Costa, Daniel,Dukhan, David,Griffe, Ludovic,Griffon, Jean-Fran?ois,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.
, p. 2634 - 2640 (2017/05/10)
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 optimization in this new series led to the identification of IDX375, a potent non-nucleoside inhibitor that is selective for genotypes 1a and 1b. The structure and binding domain of IDX375 were confirmed by X-ray co-crystalisation study.
PHOSPHADIAZINE HCV POLYMERASE INHIBITORS I AND II
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Page/Page column 53; 58, (2009/04/24)
Provided herein are phosphadiazine polymerase inhibitor, for example, of any of Formula I, II, III, I′, II′, I″, II″, Ia, IIa, or IIIa, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.
