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Page 1
Design and discovery of C2-fluoroalkyl iminothiazine dioxides as BACE inhibitors.
Taoka BM, Wu WL, Hao J, Dolmaski M, Wang H, Levorse D, Orth P, Hyde LA, Smith B, Michener MS, Kennedy ME, Parker EM, Cumming JN. Taoka BM, et al. Among authors: kennedy me. Bioorg Med Chem Lett. 2022 Jan 15;56:128463. doi: 10.1016/j.bmcl.2021.128463. Epub 2021 Nov 24. Bioorg Med Chem Lett. 2022. PMID: 34838652
Design and development of BACE-1 inhibitors.
Cumming JN, Iserloh U, Kennedy ME. Cumming JN, et al. Among authors: kennedy me. Curr Opin Drug Discov Devel. 2004 Jul;7(4):536-56. Curr Opin Drug Discov Devel. 2004. PMID: 15338962 Review.
Discovery of an orally efficaceous 4-phenoxypyrrolidine-based BACE-1 inhibitor.
Iserloh U, Pan J, Stamford AW, Kennedy ME, Zhang Q, Zhang L, Parker EM, McHugh NA, Favreau L, Strickland C, Voigt J. Iserloh U, et al. Among authors: kennedy me. Bioorg Med Chem Lett. 2008 Jan 1;18(1):418-22. doi: 10.1016/j.bmcl.2007.10.053. Epub 2007 Oct 18. Bioorg Med Chem Lett. 2008. PMID: 17980584
Potent pyrrolidine- and piperidine-based BACE-1 inhibitors.
Iserloh U, Wu Y, Cumming JN, Pan J, Wang LY, Stamford AW, Kennedy ME, Kuvelkar R, Chen X, Parker EM, Strickland C, Voigt J. Iserloh U, et al. Among authors: kennedy me. Bioorg Med Chem Lett. 2008 Jan 1;18(1):414-7. doi: 10.1016/j.bmcl.2007.10.116. Epub 2007 Nov 6. Bioorg Med Chem Lett. 2008. PMID: 18023580
Rational design of novel, potent piperazinone and imidazolidinone BACE1 inhibitors.
Cumming JN, Le TX, Babu S, Carroll C, Chen X, Favreau L, Gaspari P, Guo T, Hobbs DW, Huang Y, Iserloh U, Kennedy ME, Kuvelkar R, Li G, Lowrie J, McHugh NA, Ozgur L, Pan J, Parker EM, Saionz K, Stamford AW, Strickland C, Tadesse D, Voigt J, Wang L, Wu Y, Zhang L, Zhang Q. Cumming JN, et al. Among authors: kennedy me. Bioorg Med Chem Lett. 2008 Jun 1;18(11):3236-41. doi: 10.1016/j.bmcl.2008.04.050. Epub 2008 Apr 25. Bioorg Med Chem Lett. 2008. PMID: 18468890
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: kennedy me. J Med Chem. 2010 Feb 11;53(3):951-65. doi: 10.1021/jm901408p. J Med Chem. 2010. PMID: 20043696
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: kennedy me. J Med Chem. 2010 Feb 11;53(3):942-50. doi: 10.1021/jm901472u. J Med Chem. 2010. PMID: 20043700
Piperazine sulfonamide BACE1 inhibitors: design, synthesis, and in vivo characterization.
Cumming J, Babu S, Huang Y, Carrol C, Chen X, Favreau L, Greenlee W, Guo T, Kennedy M, Kuvelkar R, Le T, Li G, McHugh N, Orth P, Ozgur L, Parker E, Saionz K, Stamford A, Strickland C, Tadesse D, Voigt J, Zhang L, Zhang Q. Cumming J, et al. Bioorg Med Chem Lett. 2010 May 1;20(9):2837-42. doi: 10.1016/j.bmcl.2010.03.050. Epub 2010 Mar 12. Bioorg Med Chem Lett. 2010. PMID: 20347593
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: kennedy me. 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
73 results