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Page 1
Application of fragment-based lead generation to the discovery of novel, cyclic amidine beta-secretase inhibitors with nanomolar potency, cellular activity, and high ligand efficiency.
Edwards PD, Albert JS, Sylvester M, Aharony D, Andisik D, Callaghan O, Campbell JB, Carr RA, Chessari G, Congreve M, Frederickson M, Folmer RH, Geschwindner S, Koether G, Kolmodin K, Krumrine J, Mauger RC, Murray CW, Olsson LL, Patel S, Spear N, Tian G. Edwards PD, et al. J Med Chem. 2007 Nov 29;50(24):5912-25. doi: 10.1021/jm070829p. Epub 2007 Nov 7. J Med Chem. 2007. PMID: 17985862
Discovery of spirofused piperazine and diazepane amides as selective histamine-3 antagonists with in vivo efficacy in a mouse model of cognition.
Brown DG, Bernstein PR, Griffin A, Wesolowski S, Labrecque D, Tremblay MC, Sylvester M, Mauger R, Edwards PD, Throner SR, Folmer JJ, Cacciola J, Scott C, Lazor LA, Pourashraf M, Santhakumar V, Potts WM, Sydserff S, Giguère P, Lévesque C, Dasser M, Groblewski T. Brown DG, et al. J Med Chem. 2014 Feb 13;57(3):733-58. doi: 10.1021/jm4014828. Epub 2014 Jan 27. J Med Chem. 2014. PMID: 24410637
2,6-Disubstituted pyrazines and related analogs as NR2B site antagonists of the NMDA receptor with anti-depressant activity.
Brown DG, Maier DL, Sylvester MA, Hoerter TN, Menhaji-Klotz E, Lasota CC, Hirata LT, Wilkins DE, Scott CW, Trivedi S, Chen T, McCarthy DJ, Maciag CM, Sutton EJ, Cumberledge J, Mathisen D, Roberts J, Gupta A, Liu F, Elmore CS, Alhambra C, Krumrine JR, Wang X, Ciaccio PJ, Wood MW, Campbell JB, Johansson MJ, Xia J, Wen X, Jiang J, Wang X, Peng Z, Hu T, Wang J. Brown DG, et al. Among authors: sylvester ma. Bioorg Med Chem Lett. 2011 Jun 1;21(11):3399-403. doi: 10.1016/j.bmcl.2011.03.117. Epub 2011 Apr 8. Bioorg Med Chem Lett. 2011. PMID: 21524576
Discovery of efficacious Pseudomonas aeruginosa-targeted siderophore-conjugated monocarbams by application of a semi-mechanistic pharmacokinetic/pharmacodynamic model.
Murphy-Benenato KE, Bhagunde PR, Chen A, Davis HE, Durand-Réville TF, Ehmann DE, Galullo V, Harris JJ, Hatoum-Mokdad H, Jahić H, Kim A, Manjunatha MR, Manyak EL, Mueller J, Patey S, Quiroga O, Rooney M, Sha L, Shapiro AB, Sylvester M, Tan B, Tsai AS, Uria-Nickelsen M, Wu Y, Zambrowski M, Zhao SX. Murphy-Benenato KE, et al. J Med Chem. 2015 Mar 12;58(5):2195-205. doi: 10.1021/jm501506f. Epub 2015 Mar 3. J Med Chem. 2015. PMID: 25658376
Discovery of AZ0108, an orally bioavailable phthalazinone PARP inhibitor that blocks centrosome clustering.
Johannes JW, Almeida L, Daly K, Ferguson AD, Grosskurth SE, Guan H, Howard T, Ioannidis S, Kazmirski S, Lamb ML, Larsen NA, Lyne PD, Mikule K, Ogoe C, Peng B, Petteruti P, Read JA, Su N, Sylvester M, Throner S, Wang W, Wang X, Wu J, Ye Q, Yu Y, Zheng X, Scott DA. Johannes JW, et al. Bioorg Med Chem Lett. 2015 Dec 15;25(24):5743-7. doi: 10.1016/j.bmcl.2015.10.079. Epub 2015 Oct 27. Bioorg Med Chem Lett. 2015. PMID: 26546219
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