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Page 1
Synthesis and evaluation of succinoyl-caprolactam gamma-secretase inhibitors.
Thompson LA, Liauw AY, Ramanjulu MM, Kasireddy-Polam P, Mercer SE, Maduskuie TP, Glicksman M, Roach AH, Meredith JE, Liu RQ, Combs AP, Higaki JN, Cordell B, Seiffert D, Zaczek RC, Robertson DW, Olson RE. Thompson LA, et al. Bioorg Med Chem Lett. 2006 May 1;16(9):2357-63. doi: 10.1016/j.bmcl.2006.01.055. Epub 2006 Feb 10. Bioorg Med Chem Lett. 2006. PMID: 16473009
Monosubstituted γ-lactam and conformationally constrained 1,3-diaminopropan-2-ol transition-state isostere inhibitors of β-secretase (BACE).
Boy KM, Guernon JM, Shi J, Toyn JH, Meredith JE, Barten DM, Burton CR, Albright CF, Marcinkeviciene J, Good AC, Tebben AJ, Muckelbauer JK, Camac DM, Lentz KA, Bronson JJ, Olson RE, Macor JE, Thompson LA 3rd. Boy KM, et al. Among authors: thompson la 3rd. Bioorg Med Chem Lett. 2011 Nov 15;21(22):6916-24. doi: 10.1016/j.bmcl.2011.06.109. Epub 2011 Jun 30. Bioorg Med Chem Lett. 2011. PMID: 21782431
Synthesis and in vivo evaluation of cyclic diaminopropane BACE-1 inhibitors.
Thompson LA, Shi J, Decicco CP, Tebben AJ, Olson RE, Boy KM, Guernon JM, Good AC, Liauw A, Zheng C, Copeland RA, Combs AP, Trainor GL, Camac DM, Muckelbauer JK, Lentz KA, Grace JE, Burton CR, Toyn JH, Barten DM, Marcinkeviciene J, Meredith JE, Albright CF, Macor JE. Thompson LA, et al. Bioorg Med Chem Lett. 2011 Nov 15;21(22):6909-15. doi: 10.1016/j.bmcl.2011.06.116. Epub 2011 Jul 2. Bioorg Med Chem Lett. 2011. PMID: 21974952
Acyl guanidine inhibitors of β-secretase (BACE-1): optimization of a micromolar hit to a nanomolar lead via iterative solid- and solution-phase library synthesis.
Gerritz SW, Zhai W, Shi S, Zhu S, Toyn JH, Meredith JE Jr, Iben LG, Burton CR, Albright CF, Good AC, Tebben AJ, Muckelbauer JK, Camac DM, Metzler W, Cook LS, Padmanabha R, Lentz KA, Sofia MJ, Poss MA, Macor JE, Thompson LA 3rd. Gerritz SW, et al. Among authors: thompson la 3rd. J Med Chem. 2012 Nov 8;55(21):9208-23. doi: 10.1021/jm300931y. Epub 2012 Oct 2. J Med Chem. 2012. PMID: 23030502
Macrocyclic prolinyl acyl guanidines as inhibitors of β-secretase (BACE).
Boy KM, Guernon JM, Wu YJ, Zhang Y, Shi J, Zhai W, Zhu S, Gerritz SW, Toyn JH, Meredith JE, Barten DM, Burton CR, Albright CF, Good AC, Grace JE, Lentz KA, Olson RE, Macor JE, Thompson LA 3rd. Boy KM, et al. Among authors: thompson la 3rd. Bioorg Med Chem Lett. 2015 Nov 15;25(22):5040-7. doi: 10.1016/j.bmcl.2015.10.031. Epub 2015 Oct 20. Bioorg Med Chem Lett. 2015. PMID: 26497283
Design and optimization of tricyclic gamma-secretase modulators.
Shi J, Zuev D, Xu L, Lentz KA, Grace JE, Toyn JH, Olson RE, Macor JE, Thompson LA. Shi J, et al. Among authors: thompson la. Bioorg Med Chem Lett. 2016 Mar 1;26(5):1498-502. doi: 10.1016/j.bmcl.2015.06.020. Epub 2015 Jun 12. Bioorg Med Chem Lett. 2016. PMID: 26848108
Synthesis of functionalized derivatives of the gamma-secretase modulator BMS-932481 and identification of its major metabolite.
Zhang Y, Boy KM, Wu YJ, Ramirez A, Toyn JH, Ahlijanian MK, Albright CF, Zhuo X, Johnson BM, Denton RR, Olson RE, Thompson LA 3rd, Macor JE. Zhang Y, et al. Among authors: thompson la 3rd. Bioorg Med Chem Lett. 2020 Nov 15;30(22):127530. doi: 10.1016/j.bmcl.2020.127530. Epub 2020 Sep 2. Bioorg Med Chem Lett. 2020. PMID: 32890687
Presenilin-1 and -2 are molecular targets for gamma-secretase inhibitors.
Seiffert D, Bradley JD, Rominger CM, Rominger DH, Yang F, Meredith JE Jr, Wang Q, Roach AH, Thompson LA, Spitz SM, Higaki JN, Prakash SR, Combs AP, Copeland RA, Arneric SP, Hartig PR, Robertson DW, Cordell B, Stern AM, Olson RE, Zaczek R. Seiffert D, et al. Among authors: thompson la. J Biol Chem. 2000 Nov 3;275(44):34086-91. doi: 10.1074/jbc.M005430200. J Biol Chem. 2000. PMID: 10915801 Free article.
408 results