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Page 1
A Flexible, Practical, and Stereoselective Synthesis of Enantiomerically Pure trans-5-Oxohexahydropyrrolo[3,2-b]pyrroles (Pyrrolidine-trans-lactams), a New Class of Serine Protease Inhibitors, Using Acyliminium Methodology.
Macdonald SJF, Clarke GDE, Dowle MD, Harrison LA, Hodgson ST, Inglis GGA, Johnson MR, Shah P, Upton RJ, Walls SB. Macdonald SJF, et al. Among authors: harrison la. J Org Chem. 1999 Jul 9;64(14):5166-5175. doi: 10.1021/jo990306s. J Org Chem. 1999. PMID: 34237863
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. Among authors: harrison la. J Med Chem. 2002 Aug 29;45(18):3878-90. doi: 10.1021/jm020881f. J Med Chem. 2002. PMID: 12190311
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. Among authors: harrison la. 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. Among authors: harrison la. 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. Among authors: harrison la. 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 a brain-penetrant S1P₃-sparing direct agonist of the S1P₁ and S1P₅ receptors efficacious at low oral dose.
Demont EH, Arpino S, Bit RA, Campbell CA, Deeks N, Desai S, Dowell SJ, Gaskin P, Gray JR, Harrison LA, Haynes A, Heightman TD, Holmes DS, Humphreys PG, Kumar U, Morse MA, Osborne GJ, Panchal T, Philpott KL, Taylor S, Watson R, Willis R, Witherington J. Demont EH, et al. Among authors: harrison la. J Med Chem. 2011 Oct 13;54(19):6724-33. doi: 10.1021/jm200609t. Epub 2011 Sep 9. J Med Chem. 2011. PMID: 21838322
Identification of a Series of N-Methylpyridine-2-carboxamides as Potent and Selective Inhibitors of the Second Bromodomain (BD2) of the Bromo and Extra Terminal Domain (BET) Proteins.
Harrison LA, Atkinson SJ, Bassil A, Chung CW, Grandi P, Gray JRJ, Levernier E, Lewis A, Lugo D, Messenger C, Michon AM, Mitchell DJ, Preston A, Prinjha RK, Rioja I, Seal JT, Taylor S, Wall ID, Watson RJ, Woolven JM, Demont EH. Harrison LA, et al. J Med Chem. 2021 Aug 12;64(15):10742-10771. doi: 10.1021/acs.jmedchem.0c02155. Epub 2021 Jul 7. J Med Chem. 2021. PMID: 34232650
Design, Synthesis, and Characterization of I-BET567, a Pan-Bromodomain and Extra Terminal (BET) Bromodomain Oral Candidate.
Humphreys PG, Atkinson SJ, Bamborough P, Bit RA, Chung CW, Craggs PD, Cutler L, Davis R, Ferrie A, Gong G, Gordon LJ, Gray M, Harrison LA, Hayhow TG, Haynes A, Henley N, Hirst DJ, Holyer ID, Lindon MJ, Lovatt C, Lugo D, McCleary S, Molnar J, Osmani Q, Patten C, Preston A, Rioja I, Seal JT, Smithers N, Sun F, Tang D, Taylor S, Theodoulou NH, Thomas C, Watson RJ, Wellaway CR, Zhu L, Tomkinson NCO, Prinjha RK. Humphreys PG, et al. Among authors: harrison la. J Med Chem. 2022 Feb 10;65(3):2262-2287. doi: 10.1021/acs.jmedchem.1c01747. Epub 2022 Jan 7. J Med Chem. 2022. PMID: 34995458 Free article.
Template-Hopping Approach Leads to Potent, Selective, and Highly Soluble Bromo and Extraterminal Domain (BET) Second Bromodomain (BD2) Inhibitors.
Aylott HE, Atkinson SJ, Bamborough P, Bassil A, Chung CW, Gordon L, Grandi P, Gray JRJ, Harrison LA, Hayhow TG, Messenger C, Mitchell D, Phillipou A, Preston A, Prinjha RK, Rianjongdee F, Rioja I, Seal JT, Wall ID, Watson RJ, Woolven JM, Demont EH. Aylott HE, et al. Among authors: harrison la. J Med Chem. 2021 Mar 25;64(6):3249-3281. doi: 10.1021/acs.jmedchem.0c02156. Epub 2021 Mar 4. J Med Chem. 2021. PMID: 33662213
GSK973 Is an Inhibitor of the Second Bromodomains (BD2s) of the Bromodomain and Extra-Terminal (BET) Family.
Preston A, Atkinson SJ, Bamborough P, Chung CW, Gordon LJ, Grandi P, Gray JRJ, Harrison LA, Lewis AJ, Lugo D, Messenger C, Michon AM, Mitchell DJ, Prinjha RK, Rioja I, Seal J, Taylor S, Thesmar P, Wall ID, Watson RJ, Woolven JM, Demont EH. Preston A, et al. Among authors: harrison la. ACS Med Chem Lett. 2020 Jul 6;11(8):1581-1587. doi: 10.1021/acsmedchemlett.0c00247. eCollection 2020 Aug 13. ACS Med Chem Lett. 2020. PMID: 32832027 Free PMC article.
62 results