Bioorganic and Medicinal Chemistry Letters p. 2634 - 2640 (2017)
Update date:2022-07-31
Topics: Novel Discovery Experimental hepatitis C NS5B RdRp allosteric inhibitor benzophosphadiazine IDX375
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.
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.
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