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Page 1
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: dowle md. 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: dowle md. 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: dowle md. 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: dowle md. 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
The design of potent, non-peptidic inhibitors of hepatitis C protease.
Andrews DM, Chaignot HM, Coomber BA, Dowle MD, Hind SL, Johnson MR, Jones PS, Mills G, Patikis A, Pateman TJ, Robinson JE, Slater MJ, Trivedi N. Andrews DM, et al. Among authors: dowle md. Eur J Med Chem. 2003 Apr;38(4):339-43. doi: 10.1016/s0223-5234(03)00050-3. Eur J Med Chem. 2003. PMID: 12750019
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: dowle md. J Org Chem. 1999 Jul 9;64(14):5166-5175. doi: 10.1021/jo990306s. J Org Chem. 1999. PMID: 34237863
Pyrazolopyridines as potent PDE4B inhibitors: 5-heterocycle SAR.
Mitchell CJ, Ballantine SP, Coe DM, Cook CM, Delves CJ, Dowle MD, Edlin CD, Hamblin JN, Holman S, Johnson MR, Jones PS, Keeling SE, Kranz M, Lindvall M, Lucas FS, Neu M, Solanke YE, Somers DO, Trivedi NA, Wiseman JO. Mitchell CJ, et al. Among authors: dowle md. Bioorg Med Chem Lett. 2010 Oct 1;20(19):5803-6. doi: 10.1016/j.bmcl.2010.07.136. Epub 2010 Aug 5. Bioorg Med Chem Lett. 2010. PMID: 20732811
12 results