6 research outputs found
Discovery of a Potent Boronic Acid Derived Inhibitor of the HCV RNA-Dependent RNA Polymerase
A boronic acid moiety was found to
be a critical pharmacophore for enhanced in vitro potency against
wild-type hepatitis C replicons and known clinical polymorphic and
resistant HCV mutant replicons. The synthesis, optimization, and structure–activity
relationships associated with inhibition of HCV replication in a subgenomic
replication system for a series of non-nucleoside boron-containing
HCV RNA-dependent RNA polymerase (NS5B) inhibitors are described.
A summary of the discovery of <b>3</b> (GSK5852), a molecule
which entered clinical trials in subjects infected with HCV in 2011,
is included