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Discovery of cyclic acylguanidines as highly potent and selective beta-site amyloid cleaving enzyme (BACE) inhibitors: Part I--inhibitor design and validation.
Zhu Z, Sun ZY, Ye Y, Voigt J, Strickland C, Smith EM, Cumming J, Wang L, Wong J, Wang YS, Wyss DF, Chen X, Kuvelkar R, Kennedy ME, Favreau L, Parker E, McKittrick BA, Stamford A, Czarniecki M, Greenlee W, Hunter JC. Zhu Z, et al. Among authors: mckittrick ba. J Med Chem. 2010 Feb 11;53(3):951-65. doi: 10.1021/jm901408p. J Med Chem. 2010. PMID: 20043696
Discovery of potent iminoheterocycle BACE1 inhibitors.
Caldwell JP, Mazzola RD, Durkin J, Chen J, Chen X, Favreau L, Kennedy M, Kuvelkar R, Lee J, McHugh N, McKittrick B, Orth P, Stamford A, Strickland C, Voigt J, Wang L, Zhang L, Zhang Q, Zhu Z. Caldwell JP, et al. Bioorg Med Chem Lett. 2014 Dec 1;24(23):5455-9. doi: 10.1016/j.bmcl.2014.10.006. Epub 2014 Oct 23. Bioorg Med Chem Lett. 2014. PMID: 25455483
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: mckittrick ba. 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
Application of fragment-based NMR screening, X-ray crystallography, structure-based design, and focused chemical library design to identify novel microM leads for the development of nM BACE-1 (beta-site APP cleaving enzyme 1) inhibitors.
Wang YS, Strickland C, Voigt JH, Kennedy ME, Beyer BM, Senior MM, Smith EM, Nechuta TL, Madison VS, Czarniecki M, McKittrick BA, Stamford AW, Parker EM, Hunter JC, Greenlee WJ, Wyss DF. Wang YS, et al. Among authors: mckittrick ba. J Med Chem. 2010 Feb 11;53(3):942-50. doi: 10.1021/jm901472u. J Med Chem. 2010. PMID: 20043700
Structure based design of iminohydantoin BACE1 inhibitors: identification of an orally available, centrally active BACE1 inhibitor.
Cumming JN, Smith EM, Wang L, Misiaszek J, Durkin J, Pan J, Iserloh U, Wu Y, Zhu Z, Strickland C, Voigt J, Chen X, Kennedy ME, Kuvelkar R, Hyde LA, Cox K, Favreau L, Czarniecki MF, Greenlee WJ, McKittrick BA, Parker EM, Stamford AW. Cumming JN, et al. Among authors: mckittrick ba. Bioorg Med Chem Lett. 2012 Apr 1;22(7):2444-9. doi: 10.1016/j.bmcl.2012.02.013. Epub 2012 Feb 16. Bioorg Med Chem Lett. 2012. PMID: 22390835
40 results