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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: hu y. 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: hu y. 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: hu y. 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
Acylguanidine inhibitors of beta-secretase: optimization of the pyrrole ring substituents extending into the S1 and S3 substrate binding pockets.
Cole DC, Stock JR, Chopra R, Cowling R, Ellingboe JW, Fan KY, Harrison BL, Hu Y, Jacobsen S, Jennings LD, Jin G, Lohse PA, Malamas MS, Manas ES, Moore WJ, O'Donnell MM, Olland AM, Robichaud AJ, Svenson K, Wu J, Wagner E, Bard J. Cole DC, et al. Among authors: hu y. Bioorg Med Chem Lett. 2008 Feb 1;18(3):1063-6. doi: 10.1016/j.bmcl.2007.12.010. Epub 2007 Dec 10. Bioorg Med Chem Lett. 2008. PMID: 18162398
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: hu y. J Med Chem. 2008 Dec 11;51(23):7348-51. doi: 10.1021/jm801252w. J Med Chem. 2008. PMID: 19012391
Pyridinyl aminohydantoins as small molecule BACE1 inhibitors.
Zhou P, Li Y, Fan Y, Wang Z, Chopra R, Olland A, Hu Y, Magolda RL, Pangalos M, Reinhart PH, Turner MJ, Bard J, Malamas MS, Robichaud AJ. Zhou P, et al. Among authors: hu y. Bioorg Med Chem Lett. 2010 Apr 1;20(7):2326-9. doi: 10.1016/j.bmcl.2010.01.136. Epub 2010 Feb 12. Bioorg Med Chem Lett. 2010. PMID: 20202842
Novel pyrrolyl 2-aminopyridines as potent and selective human beta-secretase (BACE1) inhibitors.
Malamas MS, Barnes K, Hui Y, Johnson M, Lovering F, Condon J, Fobare W, Solvibile W, Turner J, Hu Y, Manas ES, Fan K, Olland A, Chopra R, Bard J, Pangalos MN, Reinhart P, Robichaud AJ. Malamas MS, et al. Among authors: hu y. Bioorg Med Chem Lett. 2010 Apr 1;20(7):2068-73. doi: 10.1016/j.bmcl.2010.02.075. Epub 2010 Feb 23. Bioorg Med Chem Lett. 2010. PMID: 20223661
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