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27 results

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Page 1
Preclinical profile of BI 224436, a novel HIV-1 non-catalytic-site integrase inhibitor.
Fenwick C, Amad M, Bailey MD, Bethell R, Bös M, Bonneau P, Cordingley M, Coulombe R, Duan J, Edwards P, Fader LD, Faucher AM, Garneau M, Jakalian A, Kawai S, Lamorte L, LaPlante S, Luo L, Mason S, Poupart MA, Rioux N, Schroeder P, Simoneau B, Tremblay S, Tsantrizos Y, Witvrouw M, Yoakim C. Fenwick C, et al. Among authors: jakalian a. Antimicrob Agents Chemother. 2014 Jun;58(6):3233-44. doi: 10.1128/AAC.02719-13. Epub 2014 Mar 24. Antimicrob Agents Chemother. 2014. PMID: 24663024 Free PMC article.
Discovery of BI 224436, a Noncatalytic Site Integrase Inhibitor (NCINI) of HIV-1.
Fader LD, Malenfant E, Parisien M, Carson R, Bilodeau F, Landry S, Pesant M, Brochu C, Morin S, Chabot C, Halmos T, Bousquet Y, Bailey MD, Kawai SH, Coulombe R, LaPlante S, Jakalian A, Bhardwaj PK, Wernic D, Schroeder P, Amad M, Edwards P, Garneau M, Duan J, Cordingley M, Bethell R, Mason SW, Bös M, Bonneau P, Poupart MA, Faucher AM, Simoneau B, Fenwick C, Yoakim C, Tsantrizos Y. Fader LD, et al. Among authors: jakalian a. ACS Med Chem Lett. 2014 Jan 22;5(4):422-7. doi: 10.1021/ml500002n. eCollection 2014 Apr 10. ACS Med Chem Lett. 2014. PMID: 24900852 Free PMC article.
Thiotetrazole alkynylacetanilides as potent and bioavailable non-nucleoside inhibitors of the HIV-1 wild type and K103N/Y181C double mutant reverse transcriptases.
Gagnon A, Amad MH, Bonneau PR, Coulombe R, DeRoy PL, Doyon L, Duan J, Garneau M, Guse I, Jakalian A, Jolicoeur E, Landry S, Malenfant E, Simoneau B, Yoakim C. Gagnon A, et al. Among authors: jakalian a. Bioorg Med Chem Lett. 2007 Aug 15;17(16):4437-41. doi: 10.1016/j.bmcl.2007.06.012. Epub 2007 Jun 8. Bioorg Med Chem Lett. 2007. PMID: 17583503
N-Acetamideindolecarboxylic acid allosteric 'finger-loop' inhibitors of the hepatitis C virus NS5B polymerase: discovery and initial optimization studies.
Beaulieu PL, Jolicoeur E, Gillard J, Brochu C, Coulombe R, Dansereau N, Duan J, Garneau M, Jakalian A, Kühn P, Lagacé L, LaPlante S, McKercher G, Perrault S, Poirier M, Poupart MA, Stammers T, Thauvette L, Thavonekham B, Kukolj G. Beaulieu PL, et al. Among authors: jakalian a. Bioorg Med Chem Lett. 2010 Feb 1;20(3):857-61. doi: 10.1016/j.bmcl.2009.12.101. Epub 2010 Jan 4. Bioorg Med Chem Lett. 2010. PMID: 20074949
Discovery of a novel series of non-nucleoside thumb pocket 2 HCV NS5B polymerase inhibitors.
Stammers TA, Coulombe R, Rancourt J, Thavonekham B, Fazal G, Goulet S, Jakalian A, Wernic D, Tsantrizos Y, Poupart MA, Bös M, McKercher G, Thauvette L, Kukolj G, Beaulieu PL. Stammers TA, et al. Among authors: jakalian a. Bioorg Med Chem Lett. 2013 May 1;23(9):2585-9. doi: 10.1016/j.bmcl.2013.02.110. Epub 2013 Mar 7. Bioorg Med Chem Lett. 2013. PMID: 23545108
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: jakalian a. J Med Chem. 2014 Mar 13;57(5):1845-54. doi: 10.1021/jm4011862. Epub 2013 Nov 11. J Med Chem. 2014. PMID: 24159919
Anthranilic acid-based Thumb Pocket 2 HCV NS5B polymerase inhibitors with sub-micromolar potency in the cell-based replicon assay.
Stammers TA, Coulombe R, Duplessis M, Fazal G, Gagnon A, Garneau M, Goulet S, Jakalian A, LaPlante S, Rancourt J, Thavonekham B, Wernic D, Kukolj G, Beaulieu PL. Stammers TA, et al. Among authors: jakalian a. Bioorg Med Chem Lett. 2013 Dec 15;23(24):6879-85. doi: 10.1016/j.bmcl.2013.09.102. Epub 2013 Oct 8. Bioorg Med Chem Lett. 2013. PMID: 24176401
Minimizing the Contribution of Enterohepatic Recirculation to Clearance in Rat for the NCINI Class of Inhibitors of HIV.
Fader LD, Carson R, Morin S, Bilodeau F, Chabot C, Halmos T, Bailey MD, Kawai SH, Coulombe R, Laplante S, Mekhssian K, Jakalian A, Garneau M, Duan J, Mason SW, Simoneau B, Fenwick C, Tsantrizos Y, Yoakim C. Fader LD, et al. Among authors: jakalian a. ACS Med Chem Lett. 2014 Apr 16;5(6):711-6. doi: 10.1021/ml500110j. eCollection 2014 Jun 12. ACS Med Chem Lett. 2014. PMID: 24944749 Free PMC article.
27 results