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Page 1
Design, synthesis, and in vivo characterization of a novel series of tetralin amino imidazoles as γ-secretase inhibitors: discovery of PF-3084014.
Brodney MA, Auperin DD, Becker SL, Bronk BS, Brown TM, Coffman KJ, Finley JE, Hicks CD, Karmilowicz MJ, Lanz TA, Liston D, Liu X, Martin BA, Nelson RB, Nolan CE, Oborski CE, Parker CP, Richter KE, Pozdnyakov N, Sahagan BG, Schachter JB, Sokolowski SA, Tate B, Wood DE, Wood KM, Van Deusen JW, Zhang L. Brodney MA, et al. Among authors: oborski ce. Bioorg Med Chem Lett. 2011 May 1;21(9):2637-40. doi: 10.1016/j.bmcl.2010.12.118. Epub 2010 Dec 30. Bioorg Med Chem Lett. 2011. PMID: 21269827
Thiazole-diamides as potent gamma-secretase inhibitors.
Chen YL, Cherry K, Corman ML, Ebbinghaus CF, Gamlath CB, Liston D, Martin BA, Oborski CE, Sahagan BG. Chen YL, et al. Among authors: oborski ce. Bioorg Med Chem Lett. 2007 Oct 15;17(20):5518-22. doi: 10.1016/j.bmcl.2007.08.035. Epub 2007 Aug 19. Bioorg Med Chem Lett. 2007. PMID: 17764937
Pharmacodynamics and pharmacokinetics of the gamma-secretase inhibitor PF-3084014.
Lanz TA, Wood KM, Richter KE, Nolan CE, Becker SL, Pozdnyakov N, Martin BA, Du P, Oborski CE, Wood DE, Brown TM, Finley JE, Sokolowski SA, Hicks CD, Coffman KJ, Geoghegan KF, Brodney MA, Liston D, Tate B. Lanz TA, et al. Among authors: oborski ce. J Pharmacol Exp Ther. 2010 Jul;334(1):269-77. doi: 10.1124/jpet.110.167379. Epub 2010 Apr 2. J Pharmacol Exp Ther. 2010. PMID: 20363853
Diamide amino-imidazoles: a novel series of γ-secretase inhibitors for the treatment of Alzheimer's disease.
Brodney MA, Auperin DD, Becker SL, Bronk BS, Brown TM, Coffman KJ, Finley JE, Hicks CD, Karmilowicz MJ, Lanz TA, Liston D, Liu X, Martin BA, Nelson RB, Nolan CE, Oborski CE, Parker CP, Richter KE, Pozdnyakov N, Sahagan BG, Schachter JB, Sokolowski SA, Tate B, Van Deusen JW, Wood DE, Wood KM. Brodney MA, et al. Among authors: oborski ce. Bioorg Med Chem Lett. 2011 May 1;21(9):2631-6. doi: 10.1016/j.bmcl.2010.12.117. Epub 2010 Dec 30. Bioorg Med Chem Lett. 2011. PMID: 21269825
Spirocyclic sulfamides as β-secretase 1 (BACE-1) inhibitors for the treatment of Alzheimer's disease: utilization of structure based drug design, WaterMap, and CNS penetration studies to identify centrally efficacious inhibitors.
Brodney MA, Barreiro G, Ogilvie K, Hajos-Korcsok E, Murray J, Vajdos F, Ambroise C, Christoffersen C, Fisher K, Lanyon L, Liu J, Nolan CE, Withka JM, Borzilleri KA, Efremov I, Oborski CE, Varghese A, O'Neill BT. Brodney MA, et al. Among authors: oborski ce. J Med Chem. 2012 Nov 8;55(21):9224-39. doi: 10.1021/jm3009426. Epub 2012 Oct 8. J Med Chem. 2012. PMID: 22984865
Application of the bicyclo[1.1.1]pentane motif as a nonclassical phenyl ring bioisostere in the design of a potent and orally active γ-secretase inhibitor.
Stepan AF, Subramanyam C, Efremov IV, Dutra JK, O'Sullivan TJ, DiRico KJ, McDonald WS, Won A, Dorff PH, Nolan CE, Becker SL, Pustilnik LR, Riddell DR, Kauffman GW, Kormos BL, Zhang L, Lu Y, Capetta SH, Green ME, Karki K, Sibley E, Atchison KP, Hallgren AJ, Oborski CE, Robshaw AE, Sneed B, O'Donnell CJ. Stepan AF, et al. Among authors: oborski ce. J Med Chem. 2012 Apr 12;55(7):3414-24. doi: 10.1021/jm300094u. Epub 2012 Mar 29. J Med Chem. 2012. PMID: 22420884
Discovery and optimization of a novel spiropyrrolidine inhibitor of β-secretase (BACE1) through fragment-based drug design.
Efremov IV, Vajdos FF, Borzilleri KA, Capetta S, Chen H, Dorff PH, Dutra JK, Goldstein SW, Mansour M, McColl A, Noell S, Oborski CE, O'Connell TN, O'Sullivan TJ, Pandit J, Wang H, Wei B, Withka JM. Efremov IV, et al. Among authors: oborski ce. J Med Chem. 2012 Nov 8;55(21):9069-88. doi: 10.1021/jm201715d. Epub 2012 May 9. J Med Chem. 2012. PMID: 22468999