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Page 1
Nucleotide competing reverse transcriptase inhibitors: discovery of a series of non-basic benzofurano[3,2-d]pyrimidin-2-one derived inhibitors.
James CA, DeRoy P, Duplessis M, Edwards PJ, Halmos T, Minville J, Morency L, Morin S, Simoneau B, Tremblay M, Bethell R, Cordingley M, Duan J, Lamorte L, Pelletier A, Rajotte D, Salois P, Tremblay S, Sturino CF. James CA, et al. Among authors: edwards pj. Bioorg Med Chem Lett. 2013 May 1;23(9):2781-6. doi: 10.1016/j.bmcl.2013.02.021. Epub 2013 Feb 13. Bioorg Med Chem Lett. 2013. PMID: 23545107
Identification of benzofurano[3,2-d]pyrimidin-2-ones, a new series of HIV-1 nucleotide-competing reverse transcriptase inhibitors.
Tremblay M, Bethell RC, Cordingley MG, DeRoy P, Duan J, Duplessis M, Edwards PJ, Faucher AM, Halmos T, James CA, Kuhn C, Lacoste JÉ, Lamorte L, LaPlante SR, Malenfant E, Minville J, Morency L, Morin S, Rajotte D, Salois P, Simoneau B, Tremblay S, Sturino CF. Tremblay M, et al. Among authors: edwards pj. Bioorg Med Chem Lett. 2013 May 1;23(9):2775-80. doi: 10.1016/j.bmcl.2013.02.042. Epub 2013 Feb 16. Bioorg Med Chem Lett. 2013. PMID: 23511023
Identification of potent and orally bioavailable nucleotide competing reverse transcriptase inhibitors: in vitro and in vivo optimization of a series of benzofurano[3,2-d]pyrimidin-2-one derived inhibitors.
Sturino CF, Bousquet Y, James CA, DeRoy P, Duplessis M, Edwards PJ, Halmos T, Minville J, Morency L, Morin S, Thavonekham B, Tremblay M, Duan J, Ribadeneira M, Garneau M, Pelletier A, Tremblay S, Lamorte L, Bethell R, Cordingley MG, Rajotte D, Simoneau B. Sturino CF, et al. Among authors: edwards pj. Bioorg Med Chem Lett. 2013 Jul 1;23(13):3967-75. doi: 10.1016/j.bmcl.2013.04.043. Epub 2013 Apr 25. Bioorg Med Chem Lett. 2013. PMID: 23673016
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 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. 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.
Assessing atropisomer axial chirality in drug discovery and development.
Laplante SR, D Fader L, Fandrick KR, Fandrick DR, Hucke O, Kemper R, Miller SP, Edwards PJ. Laplante SR, et al. Among authors: edwards pj. J Med Chem. 2011 Oct 27;54(20):7005-22. doi: 10.1021/jm200584g. Epub 2011 Sep 15. J Med Chem. 2011. PMID: 21848318 Review. No abstract available.
Discovery of beta-homophenylalanine based pyrrolidin-2-ylmethyl amides and sulfonamides as highly potent and selective inhibitors of dipeptidyl peptidase IV.
Nordhoff S, Cerezo-Gálvez S, Deppe H, Hill O, López-Canet M, Rummey C, Thiemann M, Matassa VG, Edwards PJ, Feurer A. Nordhoff S, et al. Among authors: edwards pj. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4201-3. doi: 10.1016/j.bmcl.2009.05.109. Epub 2009 May 30. Bioorg Med Chem Lett. 2009. PMID: 19515557
From lead to preclinical candidate: optimization of beta-homophenylalanine based inhibitors of dipeptidyl peptidase IV.
Nordhoff S, López-Canet M, Hoffmann-Enger B, Bulat S, Cerezo-Gálvez S, Hill O, Rosenbaum C, Rummey C, Thiemann M, Matassa VG, Edwards PJ, Feurer A. Nordhoff S, et al. Among authors: edwards pj. Bioorg Med Chem Lett. 2009 Aug 15;19(16):4818-23. doi: 10.1016/j.bmcl.2009.06.036. Epub 2009 Jun 13. Bioorg Med Chem Lett. 2009. PMID: 19576767
196 results