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Page 1
Profile of a Highly Selective Quaternized Pyrrolidine Betaine αvβ6 Integrin Inhibitor-(3S)-3-(3-(3,5-Dimethyl-1H-pyrazol-1-yl)phenyl)-4-((1S and 1R,3R)-1-methyl-3-(2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl)pyrrolidin-1-ium-1-yl)butanoate Synthesized by Stereoselective Methylation.
Barrett TN, Taylor JA, Barker D, Procopiou PA, Thompson JDF, Barrett J, Le J, Lynn SM, Pogany P, Pratley C, Pritchard JM, Roper JA, Rowedder JE, Slack RJ, Vitulli G, Macdonald SJF, Kerr WJ. Barrett TN, et al. Among authors: macdonald sjf. J Med Chem. 2019 Aug 22;62(16):7543-7556. doi: 10.1021/acs.jmedchem.9b00819. Epub 2019 Aug 5. J Med Chem. 2019. PMID: 31381331 Free article.
Syntheses of trans-5-oxo-hexahydro-pyrrolo[3,2-b]pyrroles and trans-5-oxo-hexahydro-furo[3,2-b]pyrroles (pyrrolidine trans-lactams and trans-lactones): new pharmacophores for elastase inhibition.
Macdonald SJ, Belton DJ, Buckley DM, Spooner JE, Anson MS, Harrison LA, Mills K, Upton RJ, Dowle MD, Smith RA, Molloy CR, Risley C. Macdonald SJ, et al. J Med Chem. 1998 Oct 8;41(21):3919-22. doi: 10.1021/jm981026s. J Med Chem. 1998. PMID: 9767628 No abstract available.
Intracellular inhibition of human neutrophil elastase by orally active pyrrolidine-trans-lactams.
Macdonald SJ, Dowle MD, Harrison LA, Spooner JE, Shah P, Johnson MR, Inglis GG, Clarke GD, Belton DJ, Smith RA, Molloy CR, Dixon M, Murkitt G, Godward RE, Skarzynski T, Singh OM, Kumar KA, Hodgson ST, McDonald E, Hardy GW, Finch H, Humphreys DC, Fleetwood G. Macdonald SJ, et al. Bioorg Med Chem Lett. 2001 Jan 22;11(2):243-6. doi: 10.1016/s0960-894x(00)00632-6. Bioorg Med Chem Lett. 2001. PMID: 11206469
The discovery of a potent, intracellular, orally bioavailable, long duration inhibitor of human neutrophil elastase--GW311616A a development candidate.
Macdonald SJ, Dowle MD, Harrison LA, Shah P, Johnson MR, Inglis GG, Clarke GD, Smith RA, Humphreys D, Molloy CR, Amour A, Dixon M, Murkitt G, Godward RE, Padfield T, Skarzynski T, Singh OM, Kumar KA, Fleetwood G, Hodgson ST, Hardy GW, Finch H. Macdonald SJ, et al. Bioorg Med Chem Lett. 2001 Apr 9;11(7):895-8. doi: 10.1016/s0960-894x(01)00078-6. Bioorg Med Chem Lett. 2001. PMID: 11294386
Discovery of further pyrrolidine trans-lactams as inhibitors of human neutrophil elastase (HNE) with potential as development candidates and the crystal structure of HNE complexed with an inhibitor (GW475151).
Macdonald SJ, Dowle MD, Harrison LA, Clarke GD, Inglis GG, Johnson MR, Shah P, Smith RA, Amour A, Fleetwood G, Humphreys DC, Molloy CR, Dixon M, Godward RE, Wonacott AJ, Singh OM, Hodgson ST, Hardy GW. Macdonald SJ, et al. J Med Chem. 2002 Aug 29;45(18):3878-90. doi: 10.1021/jm020881f. J Med Chem. 2002. PMID: 12190311
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. J Med Chem. 2005 Apr 21;48(8):2964-71. doi: 10.1021/jm040891b. J Med Chem. 2005. PMID: 15828835
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. J Med Chem. 2006 Jul 13;49(14):4216-31. doi: 10.1021/jm060302x. J Med Chem. 2006. PMID: 16821781
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. J Med Chem. 2007 Dec 27;50(26):6519-34. doi: 10.1021/jm070778w. Epub 2007 Nov 27. J Med Chem. 2007. PMID: 18038970
83 results