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Page 1
Discovery of 8-azabicyclo[3.2.1]octan-3-yloxy-benzamides as selective antagonists of the kappa opioid receptor. Part 1.
Brugel TA, Smith RW, Balestra M, Becker C, Daniels T, Hoerter TN, Koether GM, Throner SR, Panko LM, Folmer JJ, Cacciola J, Hunter AM, Liu R, Edwards PD, Brown DG, Gordon J, Ledonne NC, Pietras M, Schroeder P, Sygowski LA, Hirata LT, Zacco A, Peters MF. Brugel TA, et al. Among authors: koether gm. Bioorg Med Chem Lett. 2010 Oct 1;20(19):5847-52. doi: 10.1016/j.bmcl.2010.07.113. Epub 2010 Jul 30. Bioorg Med Chem Lett. 2010. PMID: 20727752
4-aryl piperazine and piperidine amides as novel mGluR5 positive allosteric modulators.
Xiong H, Brugel TA, Balestra M, Brown DG, Brush KA, Hightower C, Hinkley L, Hoesch V, Kang J, Koether GM, McCauley JP Jr, McLaren FM, Panko LM, Simpson TR, Smith RW, Woods JM, Brockel B, Chhajlani V, Gadient RA, Spear N, Sygowski LA, Zhang M, Arora J, Breysse N, Wilson JM, Isaac M, Slassi A, King MM. Xiong H, et al. Among authors: koether gm. Bioorg Med Chem Lett. 2010 Dec 15;20(24):7381-4. doi: 10.1016/j.bmcl.2010.10.036. Epub 2010 Oct 21. Bioorg Med Chem Lett. 2010. PMID: 21067920
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
Design, synthesis, and SAR of tachykinin antagonists: modulation of balance in NK(1)/NK(2) receptor antagonist activity.
Albert JS, Aharony D, Andisik D, Barthlow H, Bernstein PR, Bialecki RA, Dedinas R, Dembofsky BT, Hill D, Kirkland K, Koether GM, Kosmider BJ, Ohnmacht C, Palmer W, Potts W, Rumsey W, Shen L, Shenvi A, Sherwood S, Warwick PJ, Russell K. Albert JS, et al. Among authors: koether gm. J Med Chem. 2002 Aug 29;45(18):3972-83. doi: 10.1021/jm020094i. J Med Chem. 2002. PMID: 12190319
Naphtho[2,1-b][1,5] and [1,2-f][1,4]oxazocines as selective NK1 antagonists.
Ohnmacht CJ, Albert JS, Bernstein PR, Rumsey WL, Masek BB, Dembofsky BT, Koether GM, Andisik DW, Aharony D. Ohnmacht CJ, et al. Among authors: koether gm. Bioorg Med Chem. 2004 May 15;12(10):2653-69. doi: 10.1016/j.bmc.2004.03.015. Bioorg Med Chem. 2004. PMID: 15110847
Discovery of novel, orally active dual NK1/NK2 antagonists.
Bernstein PR, Aharony D, Albert JS, Andisik D, Barthlow HG, Bialecki R, Davenport T, Dedinas RF, Dembofsky BT, Koether G, Kosmider BJ, Kirkland K, Ohnmacht CJ, Potts W, Rumsey WL, Shen L, Shenvi A, Sherwood S, Stollman D, Russell K. Bernstein PR, et al. Bioorg Med Chem Lett. 2001 Oct 22;11(20):2769-73. doi: 10.1016/s0960-894x(01)00572-8. Bioorg Med Chem Lett. 2001. PMID: 11591520