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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: nomeir aa. 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
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. J Med Chem. 2012 Jan 12;55(1):489-502. doi: 10.1021/jm201407j. Epub 2011 Dec 8. J Med Chem. 2012. PMID: 22098494
Structure activity relationship studies of tricyclic bispyran sulfone γ-secretase inhibitors.
Wu WL, Asberom T, Bara T, Bennett C, Burnett DA, Clader J, Domalski M, Greenlee WJ, Josien H, McBriar M, Rajagopalan M, Vicarel M, Xu R, Hyde LA, Del Vecchio RA, Cohen-Williams ME, Song L, Lee J, Terracina G, Zhang Q, Nomeir A, Parker EM, Zhang L. Wu WL, et al. Bioorg Med Chem Lett. 2013 Feb 1;23(3):844-9. doi: 10.1016/j.bmcl.2012.11.047. Epub 2012 Nov 24. Bioorg Med Chem Lett. 2013. PMID: 23265892
Discovery of SCH 900229, a Potent Presenilin 1 Selective γ-Secretase Inhibitor for the Treatment of Alzheimer's Disease.
Wu WL, Domalski M, Burnett DA, Josien H, Bara T, Rajagopalan M, Xu R, Clader J, Greenlee WJ, Brunskill A, Hyde LA, Del Vecchio RA, Cohen-Williams ME, Song L, Lee J, Terracina G, Zhang Q, Nomeir A, Parker EM, Zhang L. Wu WL, et al. ACS Med Chem Lett. 2012 Apr 9;3(11):892-6. doi: 10.1021/ml300044f. eCollection 2012 Nov 8. ACS Med Chem Lett. 2012. PMID: 24900404 Free PMC article.
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: nomeir aa. 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
121 results