Subajini Selliah

Discovery of Novel Allosteric HCV NS5B Inhibitors. 2. Lactam-Containing Thiophene Carboxylates

Pan Li, Warren A. Dorsch, David Lauffer, Darius Bilimoria et autres

Lomibuvir ( 1 ) is a non-nucleoside, allosteric inhibitor of the hepatitis C virus NS5B polymerase with demonstrated clinical efficacy. Further development efforts within this class of inhibitor focused on improving the antiviral activity and physicochemical and pharmacokinetic properties. Recently, we reported …

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Discovery of Novel Thiophene-Based, Thumb Pocket 2 Allosteric Inhibitors of the Hepatitis C NS5B Polymerase with Improved Potency and Physicochemical Profiles

John J. Court, Carl Poisson, Andrzej Ardzinski, Darius Bilimoria et autres

The hepatitis C viral proteins NS3/4A protease, NS5B polymerase, and NS5A are clinically validated targets for direct-acting antiviral therapies. The NS5B polymerase may be inhibited directly through the action of nucleosides or nucleotide analogues or allosterically at a number of well-defined sites. …

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Discovery of thienoimidazole-based HCV NS5A inhibitors. Part 1: C2-Symmetric inhibitors with diyne and biphenyl linkers

Simon Giroux, Darius Bilimoria, Caroline Cadilhac, Kevin M. Cottrell et autres

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Discovery of thienoimidazole-based HCV NS5A inhibitors. Part 2: Non-symmetric inhibitors with potent activity against genotype 1a and 1b

Simon Giroux, Darius Bilimoria, Caroline Cadilhac, Kevin M. Cottrell et autres

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Synthesis and evaluation of NS5A inhibitors containing diverse heteroaromatic cores

James A. Henderson, Darius Bilimoria, Monica Bubenik, Caroline Cadilhac et autres

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Benzimidazole-containing HCV NS5A inhibitors: Effect of 4-substituted pyrrolidines in balancing genotype 1a and 1b potency

James A. Henderson, Darius Bilimoria, Monica Bubenik, Caroline Cadilhac et autres

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Discovery of Thienoimidazole-Based HCV NS5A Genotype 1a and 1b Inhibitors

Simon Giroux, Jinwang Xu, T. Jagadeeswar Reddy, Mark R. Morris et autres

The discovery of potent thienoimidazole-based HCV NS5A inhibitors is herein reported. A novel method to access the thienoimidazole [5,5]-bicyclic system is disclosed. This method gave access to a common key intermediate (6) that was engaged in Suzuki or Sonogashira reactions with coupling …

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Targeted impairment of innate antiviral responses in the liver of chronic hepatitis C patients

Loubna Jouan, Laurent Chatel‐Chaix, Pierre Melançon, Ian-Gaël Rodrigue-Gervais et autres

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Distinct antiviral signaling pathways in primary human hepatocytes and their differential disruption by HCV NS3 protease

Loubna Jouan, Pierre Melançon, Ian-Gaël Rodrigue-Gervais, Valérie‐Ann Raymond et autres

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961 GENOTYPIC AND PHENOTYPIC ANALYSIS OF HCV NS5B VARIANTS SELECTED FROM PATIENTS TREATED WITH VCH-916

O. Nicolas, Isabel Boivin, A. Berneche-D'Amours, P. Fex et autres

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Primary cultures of human hepatocytes isolated from hepatitis C virus‐infected cirrhotic livers as a model to study hepatitis C infection

Valérie‐Ann Raymond, Subajini Selliah, Chantal Éthier, Robert Houle et autres

BACKGROUND/AIM: Since the discovery of hepatitis C virus (HCV), researchers have encountered difficulties with in vitro models. The aim of this study was to determine whether HCV-infected human primary hepatocytes, isolated from cirrhotic livers at liver transplantation, can be used as a …

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260 Type I IFN and ISG expression in primary hepatocytes following dsRNA stimulation and expression disruption by HCV protease NS3/4A

Loubna Jouan, Pierre Melançon, Ian Gaël Rodrigue‐Gervais, Valérie‐Ann Raymond et autres

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