Design of N-Benzoxaborole Benzofuran GSK8175—Optimization of Human Pharmacokinetics Inspired by Metabolites of a Failed Clinical HCV Inhibitor

[Image: see text] We previously described the discovery of GSK5852 (1), a non-nucleoside polymerase (NS5B) inhibitor of hepatitis C virus (HCV), in which an N-benzyl boronic acid was essential for potent antiviral activity. Unfortunately, facile benzylic oxidation resulted in a short plasma half-lif...

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Bibliografiset tiedot
Julkaisussa:J Med Chem
Päätekijät: Chong, Pek Y., Shotwell, J. Brad, Miller, John, Price, Daniel J., Maynard, Andy, Voitenleitner, Christian, Mathis, Amanda, Williams, Shawn, Pouliot, Jeffrey J., Creech, Katrina, Wang, Feng, Fang, Jing, Zhang, Huichang, Tai, Vincent W.-F., Turner, Elizabeth, Kahler, Kirsten M., Crosby, Renae, Peat, Andrew J.
Aineistotyyppi: Artigo
Kieli:Inglês
Julkaistu: American Chemical Society 2019
Linkit:https://ncbi.nlm.nih.gov/pmc/articles/PMC6466479/
https://ncbi.nlm.nih.gov/pubmed/30763090
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.8b01719
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