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Discovery of novel selective norepinephrine inhibitors: 1-(2-morpholin-2-ylethyl)-3-aryl-1,3-dihydro-2,1,3-benzothiadiazole 2,2-dioxides (WYE-114152).
O'Neill DJ, Adedoyin A, Bray JA, Deecher DC, Fensome A, Goldberg JA, Harrison J, Leventhal L, Mann C, Mark L, Nogle L, Sullivan NR, Spangler TB, Terefenko EA, Trybulski EJ, Uveges AJ, Vu A, Whiteside GT, Zhang P. O'Neill DJ, et al. Among authors: terefenko ea. J Med Chem. 2011 Oct 13;54(19):6824-31. doi: 10.1021/jm200733r. Epub 2011 Sep 14. J Med Chem. 2011. PMID: 21916421
5-(3-Cyclopentyl-2-thioxo-2,3-dihydro-1H-benzimidazol-5-yl)-1-methyl-1H-pyrrole-2-carbonitrile: A novel, highly potent, selective, and orally active non-steroidal progesterone receptor agonist.
Zhang P, Terefenko E, Kern J, Fensome A, Trybulski E, Unwalla R, Wrobel J, Lockhead S, Zhu Y, Cohen J, Lacava M, Winneker RC, Zhang Z. Zhang P, et al. Among authors: terefenko e. Bioorg Med Chem. 2007 Oct 15;15(20):6556-64. doi: 10.1016/j.bmc.2007.07.011. Epub 2007 Jul 26. Bioorg Med Chem. 2007. PMID: 17681796
Structure-activity relationships of the 1-amino-3-(1H-indol-1-yl)-3-phenylpropan-2-ol series of monoamine reuptake inhibitors.
Mahaney PE, Kim CY, Coghlan RD, Cohn ST, Heffernan GD, Huselton CA, Terefenko EA, Vu AT, Zhang P, Burroughs KD, Cosmi SA, Bray JA, Johnston GH, Deecher DC, Trybulski EJ. Mahaney PE, et al. Among authors: terefenko ea. Bioorg Med Chem Lett. 2009 Oct 1;19(19):5807-10. doi: 10.1016/j.bmcl.2009.07.050. Epub 2009 Aug 25. Bioorg Med Chem Lett. 2009. PMID: 19713106
1- or 3-(3-Amino-2-hydroxy-1-phenyl propyl)-1,3-dihydro-2H-benzimidazol-2-ones: potent, selective, and orally efficacious norepinephrine reuptake inhibitors.
Zhang P, Terefenko EA, Bray J, Deecher D, Fensome A, Harrison J, Kim C, Koury E, Mark L, McComas CC, Mugford CA, Trybulski EJ, Vu AT, Whiteside GT, Mahaney PE. Zhang P, et al. Among authors: terefenko ea. J Med Chem. 2009 Sep 24;52(18):5703-11. doi: 10.1021/jm900888c. J Med Chem. 2009. PMID: 19722525
20 results