Publications by authors named "James Gillard"

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Drug Self-Aggregation into Nano-Entities Has the Potential to Induce Immune Responses.
Fatma Shahout, Marion Vanharen, Abdelaziz Saafane, James Gillard, Denis Girard

Mol Pharm· August 2023

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Discovery of Potent, Orally Bioavailable Inhibitors of Human Cytomegalovirus.
Lee Fader, Martine Brault, Jessica Desjardins, Nathalie Dansereau, Louie Lamorte, James Gillard

ACS Med Chem Lett· May 2016

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Discovery of BI 207524, an indole diamide NS5B thumb pocket 1 inhibitor with improved potency for the potential treatment of chronic hepatitis C virus infection.
Pierre L Beaulieu, Paul C Anderson, Richard Bethell, Michael Bös, Yves Bousquet, James R Gillard

J Med Chem· December 2014

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Molecular dynamics simulations and structure-based rational design lead to allosteric HCV NS5B polymerase thumb pocket 2 inhibitor with picomolar cellular replicon potency.
Oliver Hucke, René Coulombe, Pierre Bonneau, Mégan Bertrand-Laperle, Christian Brochu, James Gillard

J Med Chem· March 2014

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Enantiomeric atropisomers inhibit HCV polymerase and/or HIV matrix: characterizing hindered bond rotations and target selectivity.
Steven R LaPlante, Pat Forgione, Colette Boucher, René Coulombe, James Gillard

J Med Chem· March 2014

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Conformation-based restrictions and scaffold replacements in the design of hepatitis C virus polymerase inhibitors: discovery of deleobuvir (BI 207127).
Steven R LaPlante, Michael Bös, Christian Brochu, Catherine Chabot, René Coulombe, James R Gillard

J Med Chem· March 2014

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N- versus O-alkylation: utilizing NMR methods to establish reliable primary structure determinations for drug discovery.
Steven R LaPlante, François Bilodeau, Norman Aubry, James R Gillard, Jeff O'Meara

Bioorg Med Chem Lett· August 2013

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Compound aggregation in drug discovery: implementing a practical NMR assay for medicinal chemists.
Steven R LaPlante, Rebekah Carson, James Gillard, Norman Aubry, René Coulombe

J Med Chem· June 2013

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Discovery of the first thumb pocket 1 NS5B polymerase inhibitor (BILB 1941) with demonstrated antiviral activity in patients chronically infected with genotype 1 hepatitis C virus (HCV).
Pierre L Beaulieu, Michael Bös, Michael G Cordingley, Catherine Chabot, Gulrez Fazal, James R Gillard

J Med Chem· September 2012

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From benzimidazole to indole-5-carboxamide Thumb Pocket I inhibitors of HCV NS5B polymerase. Part 1: indole C-2 SAR and discovery of diamide derivatives with nanomolar potency in cell-based subgenomic replicons.
Pierre L Beaulieu, James Gillard, Eric Jolicoeur, Jianmin Duan, Michel Garneau

Bioorg Med Chem Lett· June 2011

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Indole 5-carboxamide Thumb Pocket I inhibitors of HCV NS5B polymerase with nanomolar potency in cell-based subgenomic replicons (part 2): central amino acid linker and right-hand-side SAR studies.
Pierre L Beaulieu, Catherine Chabot, Jianmin Duan, Michel Garneau, James Gillard

Bioorg Med Chem Lett· June 2011

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Importance of ligand bioactive conformation in the discovery of potent indole-diamide inhibitors of the hepatitis C virus NS5B.
Steven R LaPlante, James R Gillard, Araz Jakalian, Norman Aubry, René Coulombe

J Am Chem Soc· November 2010

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Benzimidazole Thumb Pocket I finger-loop inhibitors of HCV NS5B polymerase: improved drug-like properties through C-2 SAR in three sub-series.
Pierre L Beaulieu, Nathalie Dansereau, Jianmin Duan, Michel Garneau, James Gillard

Bioorg Med Chem Lett· March 2010

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N-Acetamideindolecarboxylic acid allosteric 'finger-loop' inhibitors of the hepatitis C virus NS5B polymerase: discovery and initial optimization studies.
Pierre L Beaulieu, Eric Jolicoeur, James Gillard, Christian Brochu, René Coulombe

Bioorg Med Chem Lett· February 2010

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Discovery of benzimidazole-diamide finger loop (Thumb Pocket I) allosteric inhibitors of HCV NS5B polymerase: Implementing parallel synthesis for rapid linker optimization.
Sylvie Goulet, Marc-André Poupart, James Gillard, Martin Poirier, George Kukolj

Bioorg Med Chem Lett· January 2010

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Improved replicon cellular activity of non-nucleoside allosteric inhibitors of HCV NS5B polymerase: from benzimidazole to indole scaffolds.
Pierre L Beaulieu, James Gillard, Darren Bykowski, Christian Brochu, Nathalie Dansereau

Bioorg Med Chem Lett· October 2006

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Synthesis of (1R,2S)-1-amino-2-vinylcyclopropanecarboxylic acid vinyl-ACCA) derivatives: key intermediates for the preparation of inhibitors of the hepatitis C virus NS3 protease.
Pierre L Beaulieu, James Gillard, Murray D Bailey, Colette Boucher, Jean-Simon Duceppe

J Org Chem· July 2005

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Non-nucleoside benzimidazole-based allosteric inhibitors of the hepatitis C virus NS5B polymerase: inhibition of subgenomic hepatitis C virus RNA replicons in Huh-7 cells.
Pierre L Beaulieu, Yves Bousquet, Jean Gauthier, James Gillard, Martin Marquis

J Med Chem· December 2004

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Binding mode determination of benzimidazole inhibitors of the hepatitis C virus RNA polymerase by a structure and dynamics strategy.
Steven R LaPlante, Araz Jakalian, Norman Aubry, Yves Bousquet, Jean-Marie Ferland, James Gillard

Angew Chem Int Ed Engl· August 2004

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Non-nucleoside inhibitors of the hepatitis C virus NS5B polymerase: discovery of benzimidazole 5-carboxylic amide derivatives with low-nanomolar potency.
Pierre L Beaulieu, Michael Bös, Yves Bousquet, Patrick DeRoy, Gulrez Fazal, James Gillard

Bioorg Med Chem Lett· February 2004

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Non-nucleoside inhibitors of the hepatitis C virus NS5B polymerase: discovery and preliminary SAR of benzimidazole derivatives.
Pierre L Beaulieu, Michael Bös, Yves Bousquet, Gulrez Fazal, Jean Gauthier, James Gillard

Bioorg Med Chem Lett· January 2004

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Practical Synthesis of BILA 2157 BS, a Potent and Orally Active Renin Inhibitor: Use of an Enzyme-Catalyzed Hydrolysis for the Preparation of Homochiral Succinic Acid Derivatives.
Pierre L. Beaulieu, James Gillard, Murray Bailey, Christian Beaulieu, Jean-Simon Duceppe

J Org Chem· September 1999

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