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Page 1
Discovery of (1S,2R,3S,4S,5R,6R)-2-Amino-3-[(3,4-difluorophenyl)sulfanylmethyl]-4-hydroxy-bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid Hydrochloride (LY3020371·HCl): A Potent, Metabotropic Glutamate 2/3 Receptor Antagonist with Antidepressant-Like Activity.
Chappell MD, Li R, Smith SC, Dressman BA, Tromiczak EG, Tripp AE, Blanco MJ, Vetman T, Quimby SJ, Matt J, Britton TC, Fivush AM, Schkeryantz JM, Mayhugh D, Erickson JA, Bures MG, Jaramillo C, Carpintero M, Diego JE, Barberis M, Garcia-Cerrada S, Soriano JF, Antonysamy S, Atwell S, MacEwan I, Condon B, Sougias C, Wang J, Zhang A, Conners K, Groshong C, Wasserman SR, Koss JW, Witkin JM, Li X, Overshiner C, Wafford KA, Seidel W, Wang XS, Heinz BA, Swanson S, Catlow JT, Bedwell DW, Monn JA, Mitch CH, Ornstein PL. Chappell MD, et al. Among authors: mayhugh d. J Med Chem. 2016 Dec 22;59(24):10974-10993. doi: 10.1021/acs.jmedchem.6b01119. Epub 2016 Dec 6. J Med Chem. 2016. PMID: 28002967
Discovery of the First α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic Acid (AMPA) Receptor Antagonist Dependent upon Transmembrane AMPA Receptor Regulatory Protein (TARP) γ-8.
Gardinier KM, Gernert DL, Porter WJ, Reel JK, Ornstein PL, Spinazze P, Stevens FC, Hahn P, Hollinshead SP, Mayhugh D, Schkeryantz J, Khilevich A, De Frutos O, Gleason SD, Kato AS, Luffer-Atlas D, Desai PV, Swanson S, Burris KD, Ding C, Heinz BA, Need AB, Barth VN, Stephenson GA, Diseroad BA, Woods TA, Yu H, Bredt D, Witkin JM. Gardinier KM, et al. Among authors: mayhugh d. J Med Chem. 2016 May 26;59(10):4753-68. doi: 10.1021/acs.jmedchem.6b00125. Epub 2016 Apr 29. J Med Chem. 2016. PMID: 27067148
N-(4-((2-(trifluoromethyl)-3-hydroxy-4-(isobutyryl)phenoxy)methyl)benzyl)-1-methyl-1H-imidazole-4-carboxamide (THIIC), a novel metabotropic glutamate 2 potentiator with potential anxiolytic/antidepressant properties: in vivo profiling suggests a link between behavioral and central nervous system neurochemical changes.
Fell MJ, Witkin JM, Falcone JF, Katner JS, Perry KW, Hart J, Rorick-Kehn L, Overshiner CD, Rasmussen K, Chaney SF, Benvenga MJ, Li X, Marlow DL, Thompson LK, Luecke SK, Wafford KA, Seidel WF, Edgar DM, Quets AT, Felder CC, Wang X, Heinz BA, Nikolayev A, Kuo MS, Mayhugh D, Khilevich A, Zhang D, Ebert PJ, Eckstein JA, Ackermann BL, Swanson SP, Catlow JT, Dean RA, Jackson K, Tauscher-Wisniewski S, Marek GJ, Schkeryantz JM, Svensson KA. Fell MJ, et al. Among authors: mayhugh d. J Pharmacol Exp Ther. 2011 Jan;336(1):165-77. doi: 10.1124/jpet.110.172957. Epub 2010 Oct 14. J Pharmacol Exp Ther. 2011. PMID: 20947638
Design and synthesis of new tetrahydroquinolines derivatives as CETP inhibitors.
Escribano A, Mateo AI, Martin de la Nava EM, Mayhugh DR, Cockerham SL, Beyer TP, Schmidt RJ, Cao G, Zhang Y, Jones TM, Borel AG, Sweetana SA, Cannady EA, Mantlo NB. Escribano A, et al. Among authors: mayhugh dr. Bioorg Med Chem Lett. 2012 Jun 1;22(11):3671-5. doi: 10.1016/j.bmcl.2012.04.042. Epub 2012 Apr 13. Bioorg Med Chem Lett. 2012. PMID: 22543028
Design and synthesis of a potent and selective triazolone-based peroxisome proliferator-activated receptor alpha agonist.
Xu Y, Mayhugh D, Saeed A, Wang X, Thompson RC, Dominianni SJ, Kauffman RF, Singh J, Bean JS, Bensch WR, Barr RJ, Osborne J, Montrose-Rafizadeh C, Zink RW, Yumibe NP, Huang N, Luffer-Atlas D, Rungta D, Maise DE, Mantlo NB. Xu Y, et al. Among authors: mayhugh d. J Med Chem. 2003 Nov 20;46(24):5121-4. doi: 10.1021/jm034173l. J Med Chem. 2003. PMID: 14613314
N-aryl-3,3,3-trifluoro-2-hydroxy-2-methylpropanamides: KATP potassium channel openers. Modifications on the western region.
Ohnmacht CJ, Russell K, Empfield JR, Frank CA, Gibson KH, Mayhugh DR, McLaren FM, Shapiro HS, Brown FJ, Trainor DA, Ceccarelli C, Lin MM, Masek BB, Forst JM, Harris RJ, Hulsizer JM, Lewis JJ, Silverman SM, Smith RW, Warwick PJ, Kau ST, Chun AL, Grant TL, Howe BB, Neilson KL, et al. Ohnmacht CJ, et al. Among authors: mayhugh dr. J Med Chem. 1996 Nov 8;39(23):4592-601. doi: 10.1021/jm960365n. J Med Chem. 1996. PMID: 8917648