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Page 1
Nonsteroidal glucocorticoid agonists: tetrahydronaphthalenes with alternative steroidal A-ring mimetics possessing dissociated (transrepression/transactivation) efficacy selectivity.
Biggadike K, Boudjelal M, Clackers M, Coe DM, Demaine DA, Hardy GW, Humphreys D, Inglis GG, Johnston MJ, Jones HT, House D, Loiseau R, Needham D, Skone PA, Uings I, Veitch G, Weingarten GG, McLay IM, Macdonald SJ. Biggadike K, et al. Among authors: demaine da. J Med Chem. 2007 Dec 27;50(26):6519-34. doi: 10.1021/jm070778w. Epub 2007 Nov 27. J Med Chem. 2007. PMID: 18038970
Dissociated nonsteroidal glucocorticoid receptor modulators; discovery of the agonist trigger in a tetrahydronaphthalene-benzoxazine series.
Barker M, Clackers M, Copley R, Demaine DA, Humphreys D, Inglis GG, Johnston MJ, Jones HT, Haase MV, House D, Loiseau R, Nisbet L, Pacquet F, Skone PA, Shanahan SE, Tape D, Vinader VM, Washington M, Uings I, Upton R, McLay IM, Macdonald SJ. Barker M, et al. Among authors: demaine da. J Med Chem. 2006 Jul 13;49(14):4216-31. doi: 10.1021/jm060302x. J Med Chem. 2006. PMID: 16821781
Non-steroidal glucocorticoid agonists: the discovery of aryl pyrazoles as A-ring mimetics.
Clackers M, Coe DM, Demaine DA, Hardy GW, Humphreys D, Inglis GG, Johnston MJ, Jones HT, House D, Loiseau R, Minick DJ, Skone PA, Uings I, McLay IM, Macdonald SJ. Clackers M, et al. Among authors: demaine da. Bioorg Med Chem Lett. 2007 Sep 1;17(17):4737-45. doi: 10.1016/j.bmcl.2007.06.066. Epub 2007 Jun 26. Bioorg Med Chem Lett. 2007. PMID: 17616395
Dimeric zanamivir conjugates with various linking groups are potent, long-lasting inhibitors of influenza neuraminidase including H5N1 avian influenza.
Macdonald SJ, Cameron R, Demaine DA, Fenton RJ, Foster G, Gower D, Hamblin JN, Hamilton S, Hart GJ, Hill AP, Inglis GG, Jin B, Jones HT, McConnell DB, McKimm-Breschkin J, Mills G, Nguyen V, Owens IJ, Parry N, Shanahan SE, Smith D, Watson KG, Wu WY, Tucker SP. Macdonald SJ, et al. Among authors: demaine da. J Med Chem. 2005 Apr 21;48(8):2964-71. doi: 10.1021/jm040891b. J Med Chem. 2005. PMID: 15828835
Potent and long-acting dimeric inhibitors of influenza virus neuraminidase are effective at a once-weekly dosing regimen.
Macdonald SJ, Watson KG, Cameron R, Chalmers DK, Demaine DA, Fenton RJ, Gower D, Hamblin JN, Hamilton S, Hart GJ, Inglis GG, Jin B, Jones HT, McConnell DB, Mason AM, Nguyen V, Owens IJ, Parry N, Reece PA, Shanahan SE, Smith D, Wu WY, Tucker SP. Macdonald SJ, et al. Among authors: demaine da. Antimicrob Agents Chemother. 2004 Dec;48(12):4542-9. doi: 10.1128/AAC.48.12.4542-4549.2004. Antimicrob Agents Chemother. 2004. PMID: 15561823 Free PMC article.
Cardiotonic 'C' ring modified isomazole analogues.
Barraclough P, Black JW, Cambridge D, Demaine DA, Gerskowitch VP, Giles H, Hill AP, Hull RA, Lyer R, King WR, et al. Barraclough P, et al. Among authors: demaine da. Arch Pharm (Weinheim). 1990 Aug;323(8):507-12. doi: 10.1002/ardp.19903230812. Arch Pharm (Weinheim). 1990. PMID: 2278517