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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: 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
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
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. Among authors: parker em. 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 a Novel, Potent Spirocyclic Series of γ-Secretase Inhibitors.
Zhao Z, Pissarnitski DA, Josien HB, Wu WL, Xu R, Li H, Clader JW, Burnett DA, Terracina G, Hyde L, Lee J, Song L, Zhang L, Parker EM. Zhao Z, et al. Among authors: parker em. J Med Chem. 2015 Nov 25;58(22):8806-17. doi: 10.1021/acs.jmedchem.5b00774. Epub 2015 Nov 6. J Med Chem. 2015. PMID: 26496070
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
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: parker em. 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
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
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
189 results