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34 results

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Page 1
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: barten dm. 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
N-(5-chloro-2-(hydroxymethyl)-N-alkyl-arylsulfonamides as gamma-secretase inhibitors.
Parker MF, Barten DM, Bergstrom CP, Bronson JJ, Corsa JA, Deshpande MS, Felsenstein KM, Guss VL, Hansel SB, Johnson G, Keavy DJ, Lau WY, Mock J, Prasad CV, Polson CT, Sloan CP, Smith DW, Wallace OB, Wang HH, Williams A, Zheng M. Parker MF, et al. Among authors: barten dm. Bioorg Med Chem Lett. 2007 Aug 15;17(16):4432-6. doi: 10.1016/j.bmcl.2007.06.022. Epub 2007 Jun 10. Bioorg Med Chem Lett. 2007. PMID: 17606371
Amino-caprolactam derivatives as gamma-secretase inhibitors.
Parker MF, Bronson JJ, Barten DM, Corsa JA, Du W, Felsenstein KM, Guss VL, Izzarelli D, Loo A, McElhone KE, Marcin LR, Padmanabha R, Pak R, Polson CT, Toyn JH, Varma S, Wang J, Wong V, Zheng M, Roberts SB. Parker MF, et al. Among authors: barten dm. Bioorg Med Chem Lett. 2007 Nov 1;17(21):5790-5. doi: 10.1016/j.bmcl.2007.08.047. Epub 2007 Aug 26. Bioorg Med Chem Lett. 2007. PMID: 17869509
The amyloid-beta rise and gamma-secretase inhibitor potency depend on the level of substrate expression.
Burton CR, Meredith JE, Barten DM, Goldstein ME, Krause CM, Kieras CJ, Sisk L, Iben LG, Polson C, Thompson MW, Lin XA, Corsa J, Fiedler T, Pierdomenico M, Cao Y, Roach AH, Cantone JL, Ford MJ, Drexler DM, Olson RE, Yang MG, Bergstrom CP, McElhone KE, Bronson JJ, Macor JE, Blat Y, Grafstrom RH, Stern AM, Seiffert DA, Zaczek R, Albright CF, Toyn JH. Burton CR, et al. Among authors: barten dm. J Biol Chem. 2008 Aug 22;283(34):22992-3003. doi: 10.1074/jbc.M804175200. Epub 2008 Jun 23. J Biol Chem. 2008. PMID: 18574238 Free article.
Synthesis and SAR of indole-and 7-azaindole-1,3-dicarboxamide hydroxyethylamine inhibitors of BACE-1.
Marcin LR, Higgins MA, Zusi FC, Zhang Y, Dee MF, Parker MF, Muckelbauer JK, Camac DM, Morin PE, Ramamurthy V, Tebben AJ, Lentz KA, Grace JE, Marcinkeviciene JA, Kopcho LM, Burton CR, Barten DM, Toyn JH, Meredith JE, Albright CF, Bronson JJ, Macor JE, Thompson LA. Marcin LR, et al. Among authors: barten dm. Bioorg Med Chem Lett. 2011 Jan 1;21(1):537-41. doi: 10.1016/j.bmcl.2010.10.079. Bioorg Med Chem Lett. 2011. PMID: 21078556
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. Among authors: barten dm. 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
2-(N-Benzyl-N-phenylsulfonamido)alkyl amide derivatives as γ-secretase inhibitors.
Parker MF, Barten DM, Bergstrom CP, Bronson JJ, Corsa JA, Dee MF, Gai Y, Guss VL, Higgins MA, Keavy DJ, Loo A, Mate RA, Marcin LR, McElhone KE, Polson CT, Roberts SB, Macor JE. Parker MF, et al. Among authors: barten dm. Bioorg Med Chem Lett. 2012 Nov 15;22(22):6828-31. doi: 10.1016/j.bmcl.2012.09.057. Epub 2012 Sep 24. Bioorg Med Chem Lett. 2012. PMID: 23046960
Discovery and Evaluation of BMS-708163, a Potent, Selective and Orally Bioavailable γ-Secretase Inhibitor.
Gillman KW, Starrett JE Jr, Parker MF, Xie K, Bronson JJ, Marcin LR, McElhone KE, Bergstrom CP, Mate RA, Williams R, Meredith JE Jr, Burton CR, Barten DM, Toyn JH, Roberts SB, Lentz KA, Houston JG, Zaczek R, Albright CF, Decicco CP, Macor JE, Olson RE. Gillman KW, et al. Among authors: barten dm. ACS Med Chem Lett. 2010 Mar 22;1(3):120-4. doi: 10.1021/ml1000239. eCollection 2010 Jun 10. ACS Med Chem Lett. 2010. PMID: 24900185 Free PMC article.
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: barten dm. 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
34 results