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Identification of pyridazin-3-one derivatives as potent, selective histamine H₃ receptor inverse agonists with robust wake activity.
Hudkins RL, Aimone LD, Bailey TR, Bendesky RJ, Dandu RR, Dunn D, Gruner JA, Josef KA, Lin YG, Lyons J, Marcy VR, Mathiasen JR, Sundar BG, Tao M, Zulli AL, Raddatz R, Bacon ER. Hudkins RL, et al. Among authors: bacon er. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5493-7. doi: 10.1016/j.bmcl.2011.06.108. Epub 2011 Jun 30. Bioorg Med Chem Lett. 2011. PMID: 21782432
Amine-constrained pyridazinone histamine H₃ receptor antagonists.
Sundar BG, Bailey T, Bacon E, Aimone L, Huang Z, Lyons J, Raddatz R, Hudkins R. Sundar BG, et al. Bioorg Med Chem Lett. 2011 Sep 15;21(18):5543-6. doi: 10.1016/j.bmcl.2011.06.094. Epub 2011 Jul 22. Bioorg Med Chem Lett. 2011. PMID: 21824776
Design and synthesis of dihydroindazolo[5,4-a]pyrrolo[3,4-c]carbazole oximes as potent dual inhibitors of TIE-2 and VEGF-R2 receptor tyrosine kinases.
Dandu R, Zulli AL, Bacon ER, Underiner T, Robinson C, Chang H, Miknyoczki S, Grobelny J, Ruggeri BA, Yang S, Albom MS, Angeles TS, Aimone LD, Hudkins RL. Dandu R, et al. Among authors: bacon er. Bioorg Med Chem Lett. 2008 Mar 15;18(6):1916-21. doi: 10.1016/j.bmcl.2008.02.001. Epub 2008 Feb 7. Bioorg Med Chem Lett. 2008. PMID: 18308565
Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist.
Hudkins RL, Raddatz R, Tao M, Mathiasen JR, Aimone LD, Becknell NC, Prouty CP, Knutsen LJ, Yazdanian M, Moachon G, Ator MA, Mallamo JP, Marino MJ, Bacon ER, Williams M. Hudkins RL, et al. Among authors: bacon er. J Med Chem. 2011 Jul 14;54(13):4781-92. doi: 10.1021/jm200401v. Epub 2011 Jun 2. J Med Chem. 2011. PMID: 21634396
CEP-26401 (irdabisant), a potent and selective histamine H₃ receptor antagonist/inverse agonist with cognition-enhancing and wake-promoting activities.
Raddatz R, Hudkins RL, Mathiasen JR, Gruner JA, Flood DG, Aimone LD, Le S, Schaffhauser H, Duzic E, Gasior M, Bozyczko-Coyne D, Marino MJ, Ator MA, Bacon ER, Mallamo JP, Williams M. Raddatz R, et al. Among authors: bacon er. J Pharmacol Exp Ther. 2012 Jan;340(1):124-33. doi: 10.1124/jpet.111.186585. Epub 2011 Oct 14. J Pharmacol Exp Ther. 2012. PMID: 22001260
Synthesis and biological profile of the pan-vascular endothelial growth factor receptor/tyrosine kinase with immunoglobulin and epidermal growth factor-like homology domains 2 (VEGF-R/TIE-2) inhibitor 11-(2-methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo[5,4-a]pyrrolo[3,4-c]carbazol-4-one (CEP-11981): a novel oncology therapeutic agent.
Hudkins RL, Becknell NC, Zulli AL, Underiner TL, Angeles TS, Aimone LD, Albom MS, Chang H, Miknyoczki SJ, Hunter K, Jones-Bolin S, Zhao H, Bacon ER, Mallamo JP, Ator MA, Ruggeri BA. Hudkins RL, et al. Among authors: bacon er. J Med Chem. 2012 Jan 26;55(2):903-13. doi: 10.1021/jm201449n. Epub 2012 Jan 6. J Med Chem. 2012. PMID: 22148921
Novel brain penetrant benzofuropiperidine 5-HT₆ receptor antagonists.
Sundar BG, Bailey TR, Dunn DD, Bacon ER, Salvino JM, Morton GC, Aimone LD, Zeqi H, Mathiasen JR, Dicamillo A, Huffman MJ, McKenna BA, Kopec K, Lu LD, Brown R, Qian J, Angeles T, Connors T, Spais C, Holskin B, Galinis D, Duzic E, Schaffhauser H, Rosse GC. Sundar BG, et al. Among authors: bacon er. Bioorg Med Chem Lett. 2012 Jan 1;22(1):120-3. doi: 10.1016/j.bmcl.2011.11.050. Epub 2011 Nov 22. Bioorg Med Chem Lett. 2012. PMID: 22153937
Discovery of 7-arylsulfonyl-1,2,3,4, 4a,9a-hexahydro-benzo[4,5]furo[2,3-c]pyridines: identification of a potent and selective 5-HT₆ receptor antagonist showing activity in rat social recognition test.
Tripathy R, McHugh RJ, Bacon ER, Salvino JM, Morton GC, Aimone LD, Huang Z, Mathiasen JR, DiCamillo A, Huffman MJ, McKenna BA, Kopec K, Lu LD, Qian J, Angeles TS, Connors T, Spais C, Holskin B, Duzic E, Schaffhauser H, Rossé GC. Tripathy R, et al. Among authors: bacon er. Bioorg Med Chem Lett. 2012 Feb 1;22(3):1421-6. doi: 10.1016/j.bmcl.2011.12.026. Epub 2011 Dec 13. Bioorg Med Chem Lett. 2012. PMID: 22226656
Wake-promoting agents: search for next generation modafinil: part I.
Dunn D, Hostetler G, Iqbal M, Messina-McLaughlin P, Reiboldt A, Lin YG, Gruner J, Bacon ER, Ator MA, Chatterjee S. Dunn D, et al. Among authors: bacon er. Bioorg Med Chem Lett. 2012 Mar 15;22(6):2312-4. doi: 10.1016/j.bmcl.2011.12.099. Epub 2011 Dec 29. Bioorg Med Chem Lett. 2012. PMID: 22264475
58 results