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J Med Chem. 2014 Mar 13;57(5):1902-13. doi: 10.1021/jm400317w. Epub 2013 May 29.

Discovery of a potent boronic acid derived inhibitor of the HCV RNA-dependent RNA polymerase.

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1
GlaxoSmithKline, Infectious Diseases Medicines Discovery Unit, 5 Moore Drive, Research Triangle Park, North Carolina 27709-3398, United States.

Abstract

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 3 (GSK5852), a molecule which entered clinical trials in subjects infected with HCV in 2011, is included.

PMID:
23672667
DOI:
10.1021/jm400317w
[Indexed for MEDLINE]
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