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23 results

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Page 1
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: kawai sh. 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.
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. 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 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. J Med Chem. 2014 Dec 11;57(23):10130-43. doi: 10.1021/jm501532z. Epub 2014 Nov 25. J Med Chem. 2014. PMID: 25393851
Discovery of a potent and selective noncovalent linear inhibitor of the hepatitis C virus NS3 protease (BI 201335).
Llinàs-Brunet M, Bailey MD, Goudreau N, Bhardwaj PK, Bordeleau J, Bös M, Bousquet Y, Cordingley MG, Duan J, Forgione P, Garneau M, Ghiro E, Gorys V, Goulet S, Halmos T, Kawai SH, Naud J, Poupart MA, White PW. Llinàs-Brunet M, et al. Among authors: kawai sh. J Med Chem. 2010 Sep 9;53(17):6466-76. doi: 10.1021/jm100690x. J Med Chem. 2010. PMID: 20715823
Discovery of a 1,5-dihydrobenzo[b][1,4]diazepine-2,4-dione series of inhibitors of HIV-1 capsid assembly.
Fader LD, Bethell R, Bonneau P, Bös M, Bousquet Y, Cordingley MG, Coulombe R, Deroy P, Faucher AM, Gagnon A, Goudreau N, Grand-Maître C, Guse I, Hucke O, Kawai SH, Lacoste JE, Landry S, Lemke CT, Malenfant E, Mason S, Morin S, O'Meara J, Simoneau B, Titolo S, Yoakim C. Fader LD, et al. Among authors: kawai sh. Bioorg Med Chem Lett. 2011 Jan 1;21(1):398-404. doi: 10.1016/j.bmcl.2010.10.131. Epub 2010 Oct 31. Bioorg Med Chem Lett. 2011. PMID: 21087861
Optimization of a 1,5-dihydrobenzo[b][1,4]diazepine-2,4-dione series of HIV capsid assembly inhibitors 1: addressing configurational instability through scaffold modification.
Fader LD, Landry S, Morin S, Kawai SH, Bousquet Y, Hucke O, Goudreau N, Lemke CT, Bonneau P, Titolo S, Mason S, Simoneau B. Fader LD, et al. Among authors: kawai sh. Bioorg Med Chem Lett. 2013 Jun 1;23(11):3396-400. doi: 10.1016/j.bmcl.2013.03.073. Epub 2013 Mar 28. Bioorg Med Chem Lett. 2013. PMID: 23583513
Optimization of a 1,5-dihydrobenzo[b][1,4]diazepine-2,4-dione series of HIV capsid assembly inhibitors 2: structure-activity relationships (SAR) of the C3-phenyl moiety.
Fader LD, Landry S, Goulet S, Morin S, Kawai SH, Bousquet Y, Dion I, Hucke O, Goudreau N, Lemke CT, Rancourt J, Bonneau P, Titolo S, Amad M, Garneau M, Duan J, Mason S, Simoneau B. Fader LD, et al. Among authors: kawai sh. Bioorg Med Chem Lett. 2013 Jun 1;23(11):3401-5. doi: 10.1016/j.bmcl.2013.03.074. Epub 2013 Apr 3. Bioorg Med Chem Lett. 2013. PMID: 23601710
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: kawai sh. 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.
Aligning Potency and Pharmacokinetic Properties for Pyridine-Based NCINIs.
Fader LD, Bailey M, Beaulieu E, Bilodeau F, Bonneau P, Bousquet Y, Carson RJ, Chabot C, Coulombe R, Duan J, Fenwick C, Garneau M, Halmos T, Jakalian A, James C, Kawai SH, Landry S, LaPlante SR, Mason SW, Morin S, Rioux N, Simoneau B, Surprenant S, Thavonekham B, Thibeault C, Trinh T, Tsantrizos Y, Tsoung J, Yoakim C, Wernic D. Fader LD, et al. Among authors: kawai sh. ACS Med Chem Lett. 2016 Jun 9;7(8):797-801. doi: 10.1021/acsmedchemlett.6b00194. eCollection 2016 Aug 11. ACS Med Chem Lett. 2016. PMID: 27563405 Free PMC article.
Distinct effects of two HIV-1 capsid assembly inhibitor families that bind the same site within the N-terminal domain of the viral CA protein.
Lemke CT, Titolo S, von Schwedler U, Goudreau N, Mercier JF, Wardrop E, Faucher AM, Coulombe R, Banik SS, Fader L, Gagnon A, Kawai SH, Rancourt J, Tremblay M, Yoakim C, Simoneau B, Archambault J, Sundquist WI, Mason SW. Lemke CT, et al. Among authors: kawai sh. J Virol. 2012 Jun;86(12):6643-55. doi: 10.1128/JVI.00493-12. Epub 2012 Apr 11. J Virol. 2012. PMID: 22496222 Free PMC article.
23 results