Discovery of benzophosphadiazine drug candidate IDX375: A novel hepatitis C allosteric NS5B RdRp inhibitor
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.
Direct synthesis of amino-substituted aromatic phosphonates via palladium-catalyzed coupling of aromatic mono-and dibromides with diethyl phosphite
An efficient Pd-catalyzed carbon-phosphorus bond-forming route is described for the direct synthesis of diethyl arylphosphonates bearing amino and alkylamino groups on the aromatic ring. Copyright
Bessmertnykh, Alla,Douaihy, Christiane Morkos,Guilard, Roger
supporting information; experimental part
p. 738 - 739
(2011/04/21)
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