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. 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

Andrew Maynard  1 , Renae M Crosby, Byron Ellis, Robert Hamatake, Zhi Hong, Brian A Johns, Kirsten M Kahler, Cecilia Koble, Anna Leivers, Martin R Leivers, Amanda Mathis, Andrew J Peat, Jeffrey J Pouliot, Christopher D Roberts, Vicente Samano, Rachel M Schmidt, Gary K Smith, Andrew Spaltenstein, Eugene L Stewart, Pia Thommes, Elizabeth M Turner, Christian Voitenleitner, Jill T Walker, Greg Waitt, Jason Weatherhead, Kurt Weaver, Shawn Williams, Lois Wright, Zhiping Z Xiong, David Haigh, J Brad Shotwell
Affiliations

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

Andrew Maynard et al. J Med Chem. .

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.

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