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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: zhao z. 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: zhao z. 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. Among authors: zhao z. 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: zhao z. 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: zhao z. 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
Design and synthesis of tricyclic sulfones as gamma-secretase inhibitors with greatly reduced Notch toxicity.
Xu R, Cole D, Asberom T, Bara T, Bennett C, Burnett DA, Clader J, Domalski M, Greenlee W, Hyde L, Josien H, Li H, McBriar M, McKittrick B, McPhail AT, Pissarnitski D, Qiang L, Rajagopalan M, Sasikumar T, Su J, Tang H, Wu WL, Zhang L, Zhao Z. Xu R, et al. Among authors: zhao z. Bioorg Med Chem Lett. 2010 Apr 15;20(8):2591-6. doi: 10.1016/j.bmcl.2010.02.080. Epub 2010 Feb 23. Bioorg Med Chem Lett. 2010. PMID: 20236824
Discovery of fused 5,6-bicyclic heterocycles as γ-secretase modulators.
Qin J, Dhondi P, Huang X, Mandal M, Zhao Z, Pissarnitski D, Zhou W, Aslanian R, Zhu Z, Greenlee W, Clader J, Zhang L, Cohen-Williams M, Jones N, Hyde L, Palani A. Qin J, et al. Among authors: zhao z. Bioorg Med Chem Lett. 2011 Jan 15;21(2):664-9. doi: 10.1016/j.bmcl.2010.12.012. Epub 2010 Dec 13. Bioorg Med Chem Lett. 2011. PMID: 21195610
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