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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).
Beaulieu PL, Bös M, Cordingley MG, Chabot C, Fazal G, Garneau M, Gillard JR, Jolicoeur E, LaPlante S, McKercher G, Poirier M, Poupart MA, Tsantrizos YS, Duan J, Kukolj G. Beaulieu PL, et al. Among authors: gillard jr. J Med Chem. 2012 Sep 13;55(17):7650-66. doi: 10.1021/jm3006788. Epub 2012 Aug 16. J Med Chem. 2012. PMID: 22849725
Conformation-based restrictions and scaffold replacements in the design of hepatitis C virus polymerase inhibitors: discovery of deleobuvir (BI 207127).
LaPlante SR, Bös M, Brochu C, Chabot C, Coulombe R, Gillard JR, Jakalian A, Poirier M, Rancourt J, Stammers T, Thavonekham B, Beaulieu PL, Kukolj G, Tsantrizos YS. LaPlante SR, et al. Among authors: gillard jr. J Med Chem. 2014 Mar 13;57(5):1845-54. doi: 10.1021/jm4011862. Epub 2013 Nov 11. J Med Chem. 2014. PMID: 24159919
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.
Beaulieu PL, Anderson PC, Bethell R, Bös M, Bousquet Y, Brochu C, Cordingley MG, Fazal G, Garneau M, Gillard JR, Kawai S, Marquis M, McKercher G, Poupart MA, Stammers T, Thavonekham B, Wernic D, Duan J, Kukolj G. Beaulieu PL, et al. Among authors: gillard jr. J Med Chem. 2014 Dec 11;57(23):10130-43. doi: 10.1021/jm501532z. Epub 2014 Nov 25. J Med Chem. 2014. PMID: 25393851
Improved replicon cellular activity of non-nucleoside allosteric inhibitors of HCV NS5B polymerase: from benzimidazole to indole scaffolds.
Beaulieu PL, Gillard J, Bykowski D, Brochu C, Dansereau N, Duceppe JS, Haché B, Jakalian A, Lagacé L, LaPlante S, McKercher G, Moreau E, Perreault S, Stammers T, Thauvette L, Warrington J, Kukolj G. Beaulieu PL, et al. Among authors: gillard j. Bioorg Med Chem Lett. 2006 Oct 1;16(19):4987-93. doi: 10.1016/j.bmcl.2006.07.074. Bioorg Med Chem Lett. 2006. PMID: 16908138
487 results