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252 results

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Page 1
Application of structure-based drug design and parallel chemistry to identify selective, brain penetrant, in vivo active phosphodiesterase 9A inhibitors.
Claffey MM, Helal CJ, Verhoest PR, Kang Z, Fors KS, Jung S, Zhong J, Bundesmann MW, Hou X, Lui S, Kleiman RJ, Vanase-Frawley M, Schmidt AW, Menniti F, Schmidt CJ, Hoffman WE, Hajos M, McDowell L, O'Connor RE, Macdougall-Murphy M, Fonseca KR, Becker SL, Nelson FR, Liras S. Claffey MM, et al. Among authors: becker sl. J Med Chem. 2012 Nov 8;55(21):9055-68. doi: 10.1021/jm3009635. Epub 2012 Oct 12. J Med Chem. 2012. PMID: 23025719
Metabolism-directed design of oxetane-containing arylsulfonamide derivatives as γ-secretase inhibitors.
Stepan AF, Karki K, McDonald WS, Dorff PH, Dutra JK, Dirico KJ, Won A, Subramanyam C, Efremov IV, O'Donnell CJ, Nolan CE, Becker SL, Pustilnik LR, Sneed B, Sun H, Lu Y, Robshaw AE, Riddell D, O'Sullivan TJ, Sibley E, Capetta S, Atchison K, Hallgren AJ, Miller E, Wood A, Obach RS. Stepan AF, et al. Among authors: becker sl. J Med Chem. 2011 Nov 24;54(22):7772-83. doi: 10.1021/jm200893p. Epub 2011 Oct 26. J Med Chem. 2011. PMID: 21995460
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: becker sl. J Med Chem. 2012 Apr 12;55(7):3414-24. doi: 10.1021/jm300094u. Epub 2012 Mar 29. J Med Chem. 2012. PMID: 22420884
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: becker sl. 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
Use of a physiologically based pharmacokinetic model to study the time to reach brain equilibrium: an experimental analysis of the role of blood-brain barrier permeability, plasma protein binding, and brain tissue binding.
Liu X, Smith BJ, Chen C, Callegari E, Becker SL, Chen X, Cianfrogna J, Doran AC, Doran SD, Gibbs JP, Hosea N, Liu J, Nelson FR, Szewc MA, Van Deusen J. Liu X, et al. Among authors: becker sl. J Pharmacol Exp Ther. 2005 Jun;313(3):1254-62. doi: 10.1124/jpet.104.079319. Epub 2005 Mar 2. J Pharmacol Exp Ther. 2005. PMID: 15743928
Modulation of NMDA receptor function by inhibition of D-amino acid oxidase in rodent brain.
Strick CA, Li C, Scott L, Harvey B, Hajós M, Steyn SJ, Piotrowski MA, James LC, Downs JT, Rago B, Becker SL, El-Kattan A, Xu Y, Ganong AH, Tingley FD 3rd, Ramirez AD, Seymour PA, Guanowsky V, Majchrzak MJ, Fox CB, Schmidt CJ, Duplantier AJ. Strick CA, et al. Among authors: becker sl. Neuropharmacology. 2011 Oct-Nov;61(5-6):1001-15. doi: 10.1016/j.neuropharm.2011.06.029. Epub 2011 Jul 7. Neuropharmacology. 2011. PMID: 21763704
Discovery, SAR, and pharmacokinetics of a novel 3-hydroxyquinolin-2(1H)-one series of potent D-amino acid oxidase (DAAO) inhibitors.
Duplantier AJ, Becker SL, Bohanon MJ, Borzilleri KA, Chrunyk BA, Downs JT, Hu LY, El-Kattan A, James LC, Liu S, Lu J, Maklad N, Mansour MN, Mente S, Piotrowski MA, Sakya SM, Sheehan S, Steyn SJ, Strick CA, Williams VA, Zhang L. Duplantier AJ, et al. Among authors: becker sl. J Med Chem. 2009 Jun 11;52(11):3576-85. doi: 10.1021/jm900128w. J Med Chem. 2009. PMID: 19438227
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: becker sl. 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
252 results