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Page 1
Acylguanidines as small-molecule beta-secretase inhibitors.
Cole DC, Manas ES, Stock JR, Condon JS, Jennings LD, Aulabaugh A, Chopra R, Cowling R, Ellingboe JW, Fan KY, Harrison BL, Hu Y, Jacobsen S, Jin G, Lin L, Lovering FE, Malamas MS, Stahl ML, Strand J, Sukhdeo MN, Svenson K, Turner MJ, Wagner E, Wu J, Zhou P, Bard J. Cole DC, et al. Among authors: wagner e. J Med Chem. 2006 Oct 19;49(21):6158-61. doi: 10.1021/jm0607451. J Med Chem. 2006. PMID: 17034121
Thiophene substituted acylguanidines as BACE1 inhibitors.
Fobare WF, Solvibile WR, Robichaud AJ, Malamas MS, Manas E, Turner J, Hu Y, Wagner E, Chopra R, Cowling R, Jin G, Bard J. Fobare WF, et al. Among authors: wagner e. Bioorg Med Chem Lett. 2007 Oct 1;17(19):5353-6. doi: 10.1016/j.bmcl.2007.08.010. Epub 2007 Aug 11. Bioorg Med Chem Lett. 2007. PMID: 17761418
Acylguanidine inhibitors of beta-secretase: optimization of the pyrrole ring substituents extending into the S1' substrate binding pocket.
Jennings LD, Cole DC, Stock JR, Sukhdeo MN, Ellingboe JW, Cowling R, Jin G, Manas ES, Fan KY, Malamas MS, Harrison BL, Jacobsen S, Chopra R, Lohse PA, Moore WJ, O'Donnell MM, Hu Y, Robichaud AJ, Turner MJ, Wagner E, Bard J. Jennings LD, et al. Among authors: wagner e. Bioorg Med Chem Lett. 2008 Jan 15;18(2):767-71. doi: 10.1016/j.bmcl.2007.11.043. Epub 2007 Nov 17. Bioorg Med Chem Lett. 2008. PMID: 18068983
Discovery of begacestat, a Notch-1-sparing gamma-secretase inhibitor for the treatment of Alzheimer's disease.
Mayer SC, Kreft AF, Harrison B, Abou-Gharbia M, Antane M, Aschmies S, Atchison K, Chlenov M, Cole DC, Comery T, Diamantidis G, Ellingboe J, Fan K, Galante R, Gonzales C, Ho DM, Hoke ME, Hu Y, Huryn D, Jain U, Jin M, Kremer K, Kubrak D, Lin M, Lu P, Magolda R, Martone R, Moore W, Oganesian A, Pangalos MN, Porte A, Reinhart P, Resnick L, Riddell DR, Sonnenberg-Reines J, Stock JR, Sun SC, Wagner E, Wang T, Woller K, Xu Z, Zaleska MM, Zeldis J, Zhang M, Zhou H, Jacobsen JS. Mayer SC, et al. Among authors: wagner e. J Med Chem. 2008 Dec 11;51(23):7348-51. doi: 10.1021/jm801252w. J Med Chem. 2008. PMID: 19012391
Discovery and initial optimization of 5,5'-disubstituted aminohydantoins as potent beta-secretase (BACE1) inhibitors.
Nowak P, Cole DC, Aulabaugh A, Bard J, Chopra R, Cowling R, Fan KY, Hu B, Jacobsen S, Jani M, Jin G, Lo MC, Malamas MS, Manas ES, Narasimhan R, Reinhart P, Robichaud AJ, Stock JR, Subrath J, Svenson K, Turner J, Wagner E, Zhou P, Ellingboe JW. Nowak P, et al. Among authors: wagner e. Bioorg Med Chem Lett. 2010 Jan 15;20(2):632-5. doi: 10.1016/j.bmcl.2009.11.052. Epub 2009 Nov 20. Bioorg Med Chem Lett. 2010. PMID: 19959359
Design and synthesis of aminohydantoins as potent and selective human β-secretase (BACE1) inhibitors with enhanced brain permeability.
Malamas MS, Robichaud A, Erdei J, Quagliato D, Solvibile W, Zhou P, Morris K, Turner J, Wagner E, Fan K, Olland A, Jacobsen S, Reinhart P, Riddell D, Pangalos M. Malamas MS, et al. Among authors: wagner e. Bioorg Med Chem Lett. 2010 Nov 15;20(22):6597-605. doi: 10.1016/j.bmcl.2010.09.029. Epub 2010 Sep 15. Bioorg Med Chem Lett. 2010. PMID: 20880704
Discovery of a novel series of Notch-sparing gamma-secretase inhibitors.
Kreft A, Harrison B, Aschmies S, Atchison K, Casebier D, Cole DC, Diamantidis G, Ellingboe J, Hauze D, Hu Y, Huryn D, Jin M, Kubrak D, Lu P, Lundquist J, Mann C, Martone R, Moore W, Oganesian A, Porte A, Riddell DR, Sonnenberg-Reines J, Stock JR, Sun SC, Wagner E, Woller K, Xu Z, Zhou H, Steven Jacobsen J. Kreft A, et al. Among authors: wagner e. Bioorg Med Chem Lett. 2008 Jul 15;18(14):4232-6. doi: 10.1016/j.bmcl.2008.05.064. Epub 2008 May 20. Bioorg Med Chem Lett. 2008. PMID: 18556202
3,275 results