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Page 1
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. Among authors: orth p. 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 and activity relationships of tartrate-based TACE inhibitors.
Li D, Popovici-Muller J, Belanger DB, Caldwell J, Dai C, David M, Girijavallabhan VM, Lavey BJ, Lee JF, Liu Z, Mazzola R, Rizvi R, Rosner KE, Shankar B, Spitler J, Ting PC, Vaccaro H, Yu W, Zhou G, Zhu Z, Niu X, Sun J, Guo Z, Orth P, Chen S, Kozlowski JA, Lundell DJ, Madison V, McKittrick B, Piwinski JJ, Shih NY, Shipps GW Jr, Siddiqui MA, Strickland CO. Li D, et al. Among authors: orth p. Bioorg Med Chem Lett. 2010 Aug 15;20(16):4812-5. doi: 10.1016/j.bmcl.2010.06.104. Epub 2010 Jun 25. Bioorg Med Chem Lett. 2010. PMID: 20638281
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: orth p. 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.
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. Among authors: orth p. 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
Discovery and optimization of antibacterial AccC inhibitors.
Cheng CC, Shipps GW Jr, Yang Z, Sun B, Kawahata N, Soucy KA, Soriano A, Orth P, Xiao L, Mann P, Black T. Cheng CC, et al. Among authors: orth p. Bioorg Med Chem Lett. 2009 Dec 1;19(23):6507-14. doi: 10.1016/j.bmcl.2009.10.057. Epub 2009 Oct 28. Bioorg Med Chem Lett. 2009. PMID: 19875284
Iminopyrimidinones: a novel pharmacophore for the development of orally active renin inhibitors.
McKittrick BA, Caldwell JP, Bara T, Boykow G, Chintala M, Clader J, Czarniecki M, Courneya B, Duffy R, Fleming L, Giessert R, Greenlee WJ, Heap C, Hong L, Huang Y, Iserloh U, Josien H, Khan T, Korfmacher W, Liang X, Mazzola R, Mitra S, Moore K, Orth P, Rajagopalan M, Roy S, Sakwa S, Strickland C, Vaccaro H, Voigt J, Wang H, Wong J, Zhang R, Zych A. McKittrick BA, et al. Among authors: orth p. Bioorg Med Chem Lett. 2015 Apr 1;25(7):1592-6. doi: 10.1016/j.bmcl.2015.02.003. Epub 2015 Feb 10. Bioorg Med Chem Lett. 2015. PMID: 25728416
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: orth p. 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-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: orth p. 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
The discovery of novel tartrate-based TNF-alpha converting enzyme (TACE) inhibitors.
Rosner KE, Guo Z, Orth P, Shipps GW Jr, Belanger DB, Chan TY, Curran PJ, Dai C, Deng Y, Girijavallabhan VM, Hong L, Lavey BJ, Lee JF, Li D, Liu Z, Popovici-Muller J, Ting PC, Vaccaro H, Wang L, Wang T, Yu W, Zhou G, Niu X, Sun J, Kozlowski JA, Lundell DJ, Madison V, McKittrick B, Piwinski JJ, Shih NY, Arshad Siddiqui M, Strickland CO. Rosner KE, et al. Among authors: orth p. Bioorg Med Chem Lett. 2010 Feb 1;20(3):1189-93. doi: 10.1016/j.bmcl.2009.12.004. Epub 2009 Dec 5. Bioorg Med Chem Lett. 2010. PMID: 20022498
156 results