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Page 1
Synthesis and biological evaluation of benzodioxanylpiperazine derivatives as potent serotonin 5-HT(1A) antagonists: the discovery of Lecozotan.
Childers WE Jr, Abou-Gharbia MA, Kelly MG, Andree TH, Harrison BL, Ho DM, Hornby G, Huryn DM, Potestio L, Rosenzweig-Lipson SJ, Schmid J, Smith DL, Sukoff SJ, Zhang G, Schechter LE. Childers WE Jr, et al. Among authors: kelly mg. J Med Chem. 2005 May 19;48(10):3467-70. doi: 10.1021/jm049493z. J Med Chem. 2005. PMID: 15887953
Correlating efficacy in rodent cognition models with in vivo 5-hydroxytryptamine1a receptor occupancy by a novel antagonist, (R)-N-(2-methyl-(4-indolyl-1-piperazinyl)ethyl)-N-(2-pyridinyl)-cyclohexane carboxamide (WAY-101405).
Hirst WD, Andree TH, Aschmies S, Childers WE, Comery TA, Dawson LA, Day M, Feingold IB, Grauer SM, Harrison BL, Hughes ZA, Kao J, Kelly MG, van der Lee H, Rosenzweig-Lipson S, Saab AL, Smith DL, Sullivan K, Rizzo SJ, Tio C, Zhang MY, Schechter LE. Hirst WD, et al. Among authors: kelly mg. J Pharmacol Exp Ther. 2008 Apr;325(1):134-45. doi: 10.1124/jpet.107.133082. Epub 2008 Jan 8. J Pharmacol Exp Ther. 2008. PMID: 18182558
Melanocortin subtype-4 receptor agonists containing a piperazine core with substituted aryl sulfonamides.
Fotsch C, Han N, Arasasingham P, Bo Y, Carmouche M, Chen N, Davis J, Goldberg MH, Hale C, Hsieh FY, Kelly MG, Liu Q, Norman MH, Smith DM, Stec M, Tamayo N, Xi N, Xu S, Bannon AW, Baumgartner JW. Fotsch C, et al. Among authors: kelly mg. Bioorg Med Chem Lett. 2005 Mar 15;15(6):1623-7. doi: 10.1016/j.bmcl.2005.01.060. Bioorg Med Chem Lett. 2005. PMID: 15745810
Identification of orally-bioavailable antagonists of the TRPV4 ion-channel.
Wei ZL, Nguyen MT, O'Mahony DJ, Acevedo A, Zipfel S, Zhang Q, Liu L, Dourado M, Chi C, Yip V, DeFalco J, Gustafson A, Emerling DE, Kelly MG, Kincaid J, Vincent F, Duncton MA. Wei ZL, et al. Among authors: kelly mg. Bioorg Med Chem Lett. 2015 Sep 15;25(18):4011-5. doi: 10.1016/j.bmcl.2015.06.098. Epub 2015 Jul 6. Bioorg Med Chem Lett. 2015. PMID: 26235950
Design of a new peptidomimetic agonist for the melanocortin receptors based on the solution structure of the peptide ligand, Ac-Nle-cyclo[Asp-Pro-DPhe-Arg-Trp-Lys]-NH(2).
Fotsch C, Smith DM, Adams JA, Cheetham J, Croghan M, Doherty EM, Hale C, Jarosinski MA, Kelly MG, Norman MH, Tamayo NA, Xi N, Baumgartner JW. Fotsch C, et al. Among authors: kelly mg. Bioorg Med Chem Lett. 2003 Jul 21;13(14):2337-40. doi: 10.1016/s0960-894x(03)00412-8. Bioorg Med Chem Lett. 2003. PMID: 12824029
159 results