Discovery of a Potent Boronic Acid Derived Inhibitor of the HCV RNA-Dependent RNA Polymerase
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14/05/2013
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| Resumo |
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 sub-genomic 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 GSK5852 (3), a molecule which entered clinical trials in subjects infected with HCV in 2011, is included. |
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| Idioma(s) |
eng |
| Direitos |
info:eu-repo/semantics/restrictedAccess |
| Fonte |
Maynard , A , Crosby , R M , Ellis , B , Hamatake , R , Hong , Z , Johns , B A , Kahler , K M , Koble , C , Leivers , A L , Leivers , M R , Mathis , A , Peat , A J , Pouliot , J J , Roberts , C D , Samano , V , Schmidt , R M , Smith , G K , Spaltenstein , A , Stewart , E L , Thommes , P , Turner , E M , Voitenleitner , C , Walker , J T , Waitt , G , Weatherhead , J , Weaver , K L , Williams , S , Wright , L , Xiong , Z Z , Haigh , D & Shotwell , J B 2013 , ' Discovery of a Potent Boronic Acid Derived Inhibitor of the HCV RNA-Dependent RNA Polymerase ' Journal of Medicinal Chemistry . DOI: 10.1021/jm400317w |
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article |
