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Page 1
Cyclic hydroxyamidines as amide isosteres: discovery of oxadiazolines and oxadiazines as potent and highly efficacious γ-secretase modulators in vivo.
Sun ZY, Asberom T, Bara T, Bennett C, Burnett D, Chu I, Clader J, Cohen-Williams M, Cole D, Czarniecki M, Durkin J, Gallo G, Greenlee W, Josien H, Huang X, Hyde L, Jones N, Kazakevich I, Li H, Liu X, Lee J, Maccoss M, Mandal MB, McCracken T, Nomeir A, Mazzola R, Palani A, Parker EM, Pissarnitski DA, Qin J, Song L, Terracina G, Vicarel M, Voigt J, Xu R, Zhang L, Zhang Q, Zhao Z, Zhu X, Zhu Z. Sun ZY, et al. Among authors: pissarnitski da. J Med Chem. 2012 Jan 12;55(1):489-502. doi: 10.1021/jm201407j. Epub 2011 Dec 8. J Med Chem. 2012. PMID: 22098494
Tetrahydroquinoline sulfonamides as gamma-secretase inhibitors.
Asberom T, Bara TA, Clader JW, Greenlee WJ, Guzik HS, Josien HB, Li W, Parker EM, Pissarnitski DA, Song L, Zhang L, Zhao Z. Asberom T, et al. Among authors: pissarnitski da. Bioorg Med Chem Lett. 2007 Jan 1;17(1):205-7. doi: 10.1016/j.bmcl.2006.09.064. Epub 2006 Oct 12. Bioorg Med Chem Lett. 2007. PMID: 17046254
2,6-Disubstituted N-arylsulfonyl piperidines as gamma-secretase inhibitors.
Pissarnitski DA, Asberom T, Bara TA, Buevich AV, Clader JW, Greenlee WJ, Guzik HS, Josien HB, Li W, McEwan M, McKittrick BA, Nechuta TL, Parker EM, Sinning L, Smith EM, Song L, Vaccaro HA, Voigt JH, Zhang L, Zhang Q, Zhao Z. Pissarnitski DA, et al. Bioorg Med Chem Lett. 2007 Jan 1;17(1):57-62. doi: 10.1016/j.bmcl.2006.09.094. Epub 2006 Oct 4. Bioorg Med Chem Lett. 2007. PMID: 17055268
Discovery of gamma-secretase inhibitors efficacious in a transgenic animal model of Alzheimer's disease.
Asberom T, Zhao Z, Bara TA, Clader JW, Greenlee WJ, Hyde LA, Josien HB, Li W, McPhail AT, Nomeir AA, Parker EM, Rajagopalan M, Song L, Wong GT, Zhang L, Zhang Q, Pissarnitski DA. Asberom T, et al. Among authors: pissarnitski da. Bioorg Med Chem Lett. 2007 Jan 15;17(2):511-6. doi: 10.1016/j.bmcl.2006.10.011. Epub 2006 Oct 10. Bioorg Med Chem Lett. 2007. PMID: 17079141
Small conformationally restricted piperidine N-arylsulfonamides as orally active gamma-secretase inhibitors.
Josien H, Bara T, Rajagopalan M, Asberom T, Clader JW, Favreau L, Greenlee WJ, Hyde LA, Nomeir AA, Parker EM, Pissarnitski DA, Song L, Wong GT, Zhang L, Zhang Q, Zhao Z. Josien H, et al. Among authors: pissarnitski da. Bioorg Med Chem Lett. 2007 Oct 1;17(19):5330-5. doi: 10.1016/j.bmcl.2007.08.013. Epub 2007 Aug 15. Bioorg Med Chem Lett. 2007. PMID: 17761417
Discovery of 2,4,6-trisubstituted N-arylsulfonyl piperidines as gamma-secretase inhibitors.
Li H, Asberom T, Bara TA, Clader JW, Greenlee WJ, Josien HB, McBriar MD, Nomeir A, Pissarnitski DA, Rajagopalan M, Xu R, Zhao Z, Song L, Zhang L. Li H, et al. Among authors: pissarnitski da. Bioorg Med Chem Lett. 2007 Nov 15;17(22):6290-4. doi: 10.1016/j.bmcl.2007.09.006. Epub 2007 Sep 7. Bioorg Med Chem Lett. 2007. PMID: 17890085
Discovery of amide and heteroaryl isosteres as carbamate replacements in a series of orally active gamma-secretase inhibitors.
McBriar MD, Clader JW, Chu I, Del Vecchio RA, Favreau L, Greenlee WJ, Hyde LA, Nomeir AA, Parker EM, Pissarnitski DA, Song L, Zhang L, Zhao Z. McBriar MD, et al. Among authors: pissarnitski da. Bioorg Med Chem Lett. 2008 Jan 1;18(1):215-9. doi: 10.1016/j.bmcl.2007.10.092. Epub 2007 Oct 30. Bioorg Med Chem Lett. 2008. PMID: 17988864
Discovery of a Novel, Potent Spirocyclic Series of γ-Secretase Inhibitors.
Zhao Z, Pissarnitski DA, Josien HB, Wu WL, Xu R, Li H, Clader JW, Burnett DA, Terracina G, Hyde L, Lee J, Song L, Zhang L, Parker EM. Zhao Z, et al. Among authors: pissarnitski da. J Med Chem. 2015 Nov 25;58(22):8806-17. doi: 10.1021/acs.jmedchem.5b00774. Epub 2015 Nov 6. J Med Chem. 2015. PMID: 26496070
Substituted 4-morpholine N-arylsulfonamides as γ-secretase inhibitors.
Zhao Z, Pissarnitski DA, Josien HB, Bara TA, Clader JW, Li H, McBriar MD, Rajagopalan M, Xu R, Terracina G, Hyde L, Song L, Zhang L, Parker EM, Osterman R, Buevich AV. Zhao Z, et al. Among authors: pissarnitski da. Eur J Med Chem. 2016 Nov 29;124:36-48. doi: 10.1016/j.ejmech.2016.08.024. Epub 2016 Aug 13. Eur J Med Chem. 2016. PMID: 27560281
30 results