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192 results

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Page 1
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: parker em. 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
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: parker em. 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: parker em. 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
Design and validation of bicyclic iminopyrimidinones as beta amyloid cleaving enzyme-1 (BACE1) inhibitors: conformational constraint to favor a bioactive conformation.
Mandal M, Zhu Z, Cumming JN, Liu X, Strickland C, Mazzola RD, Caldwell JP, Leach P, Grzelak M, Hyde L, Zhang Q, Terracina G, Zhang L, Chen X, Kuvelkar R, Kennedy ME, Favreau L, Cox K, Orth P, Buevich A, Voigt J, Wang H, Kazakevich I, McKittrick BA, Greenlee W, Parker EM, Stamford AW. Mandal M, et al. Among authors: parker em. J Med Chem. 2012 Nov 8;55(21):9331-45. doi: 10.1021/jm301039c. Epub 2012 Oct 1. J Med Chem. 2012. PMID: 22989333
Discovery of an Orally Available, Brain Penetrant BACE1 Inhibitor that Affords Robust CNS Aβ Reduction.
Stamford AW, Scott JD, Li SW, Babu S, Tadesse D, Hunter R, Wu Y, Misiaszek J, Cumming JN, Gilbert EJ, Huang C, McKittrick BA, Hong L, Guo T, Zhu Z, Strickland C, Orth P, Voigt JH, Kennedy ME, Chen X, Kuvelkar R, Hodgson R, Hyde LA, Cox K, Favreau L, Parker EM, Greenlee WJ. Stamford AW, et al. Among authors: parker em. ACS Med Chem Lett. 2012 Nov 8;3(11):897-902. doi: 10.1021/ml3001165. Epub 2012 Jul 12. ACS Med Chem Lett. 2012. PMID: 23412139 Free PMC article.
Structure-Based Design of an Iminoheterocyclic β-Site Amyloid Precursor Protein Cleaving Enzyme (BACE) Inhibitor that Lowers Central Aβ in Nonhuman Primates.
Mandal M, Wu Y, Misiaszek J, Li G, Buevich A, Caldwell JP, Liu X, Mazzola RD, Orth P, Strickland C, Voigt J, Wang H, Zhu Z, Chen X, Grzelak M, Hyde LA, Kuvelkar R, Leach PT, Terracina G, Zhang L, Zhang Q, Michener MS, Smith B, Cox K, Grotz D, Favreau L, Mitra K, Kazakevich I, McKittrick BA, Greenlee W, Kennedy ME, Parker EM, Cumming JN, Stamford AW. Mandal M, et al. Among authors: parker em. J Med Chem. 2016 Apr 14;59(7):3231-48. doi: 10.1021/acs.jmedchem.5b01995. Epub 2016 Mar 22. J Med Chem. 2016. PMID: 26937601
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: parker em. 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
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: parker em. 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: parker em. 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
192 results