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247 results

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Page 1
Design and development of a series of borocycles as selective, covalent kallikrein 5 inhibitors.
Walker AL, Denis A, Bingham RP, Bouillot A, Edgar EV, Ferrie A, Holmes DS, Laroze A, Liddle J, Fouchet MH, Moquette A, Nassau P, Pearce AC, Polyakova O, Smith KJ, Thomas P, Thorpe JH, Trottet L, Wang Y, Hovnanian A. Walker AL, et al. Among authors: holmes ds. Bioorg Med Chem Lett. 2019 Oct 15;29(20):126675. doi: 10.1016/j.bmcl.2019.126675. Epub 2019 Sep 7. Bioorg Med Chem Lett. 2019. PMID: 31521475
Biphenyl amide p38 kinase inhibitors 3: Improvement of cellular and in vivo activity.
Angell R, Aston NM, Bamborough P, Buckton JB, Cockerill S, deBoeck SJ, Edwards CD, Holmes DS, Jones KL, Laine DI, Patel S, Smee PA, Smith KJ, Somers DO, Walker AL. Angell R, et al. Among authors: holmes ds. Bioorg Med Chem Lett. 2008 Aug 1;18(15):4428-32. doi: 10.1016/j.bmcl.2008.06.048. Epub 2008 Jun 18. Bioorg Med Chem Lett. 2008. PMID: 18614366
4-Phenyl-7-azaindoles as potent and selective IKK2 inhibitors.
Liddle J, Bamborough P, Barker MD, Campos S, Cousins RP, Cutler GJ, Hobbs H, Holmes DS, Ioannou C, Mellor GW, Morse MA, Payne JJ, Pritchard JM, Smith KJ, Tape DT, Whitworth C, Williamson RA. Liddle J, et al. Among authors: holmes ds. Bioorg Med Chem Lett. 2009 May 1;19(9):2504-8. doi: 10.1016/j.bmcl.2009.03.034. Epub 2009 Mar 14. Bioorg Med Chem Lett. 2009. PMID: 19349179
Quinolines as a novel structural class of potent and selective PDE4 inhibitors. Optimisation for inhaled administration.
Woodrow MD, Ballantine SP, Barker MD, Clarke BJ, Dawson J, Dean TW, Delves CJ, Evans B, Gough SL, Guntrip SB, Holman S, Holmes DS, Kranz M, Lindvaal MK, Lucas FS, Neu M, Ranshaw LE, Solanke YE, Somers DO, Ward P, Wiseman JO. Woodrow MD, et al. Among authors: holmes ds. Bioorg Med Chem Lett. 2009 Sep 1;19(17):5261-5. doi: 10.1016/j.bmcl.2009.04.012. Epub 2009 Apr 9. Bioorg Med Chem Lett. 2009. PMID: 19656678
Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating metabolic inactivation: an antedrug approach.
Procopiou PA, Barrett VJ, Bevan NJ, Biggadike K, Box PC, Butchers PR, Coe DM, Conroy R, Emmons A, Ford AJ, Holmes DS, Horsley H, Kerr F, Li-Kwai-Cheung AM, Looker BE, Mann IS, McLay IM, Morrison VS, Mutch PJ, Smith CE, Tomlin P. Procopiou PA, et al. Among authors: holmes ds. J Med Chem. 2010 Jun 10;53(11):4522-30. doi: 10.1021/jm100326d. J Med Chem. 2010. PMID: 20462258
The discovery of phthalazinone-based human H1 and H3 single-ligand antagonists suitable for intranasal administration for the treatment of allergic rhinitis.
Procopiou PA, Browning C, Buckley JM, Clark KL, Fechner L, Gore PM, Hancock AP, Hodgson ST, Holmes DS, Kranz M, Looker BE, Morriss KM, Parton DL, Russell LJ, Slack RJ, Sollis SL, Vile S, Watts CJ. Procopiou PA, et al. Among authors: holmes ds. J Med Chem. 2011 Apr 14;54(7):2183-95. doi: 10.1021/jm1013874. Epub 2011 Mar 7. J Med Chem. 2011. PMID: 21381763
4-Phenyl-7-azaindoles as potent, selective and bioavailable IKK2 inhibitors demonstrating good in vivo efficacy.
Liddle J, Bamborough P, Barker MD, Campos S, Chung CW, Cousins RP, Faulder P, Heathcote ML, Hobbs H, Holmes DS, Ioannou C, Ramirez-Molina C, Morse MA, Osborn R, Payne JJ, Pritchard JM, Rumsey WL, Tape DT, Vicentini G, Whitworth C, Williamson RA. Liddle J, et al. Among authors: holmes ds. Bioorg Med Chem Lett. 2012 Aug 15;22(16):5222-6. doi: 10.1016/j.bmcl.2012.06.065. Epub 2012 Jun 26. Bioorg Med Chem Lett. 2012. PMID: 22801646
Discovery of Tetrahydropyrazolopyridine as Sphingosine 1-Phosphate Receptor 3 (S1P3)-Sparing S1P1 Agonists Active at Low Oral Doses.
Demont EH, Bailey JM, Bit RA, Brown JA, Campbell CA, Deeks N, Dowell SJ, Eldred C, Gaskin P, Gray JR, Haynes A, Hirst DJ, Holmes DS, Kumar U, Morse MA, Osborne GJ, Renaux JF, Seal GA, Smethurst CA, Taylor S, Watson R, Willis R, Witherington J. Demont EH, et al. Among authors: holmes ds. J Med Chem. 2016 Feb 11;59(3):1003-20. doi: 10.1021/acs.jmedchem.5b01512. Epub 2016 Jan 22. J Med Chem. 2016. PMID: 26751273
Kynurenine-3-monooxygenase inhibition prevents multiple organ failure in rodent models of acute pancreatitis.
Mole DJ, Webster SP, Uings I, Zheng X, Binnie M, Wilson K, Hutchinson JP, Mirguet O, Walker A, Beaufils B, Ancellin N, Trottet L, Bénéton V, Mowat CG, Wilkinson M, Rowland P, Haslam C, McBride A, Homer NZ, Baily JE, Sharp MG, Garden OJ, Hughes J, Howie SE, Holmes DS, Liddle J, Iredale JP. Mole DJ, et al. Among authors: holmes ds. Nat Med. 2016 Feb;22(2):202-9. doi: 10.1038/nm.4020. Epub 2016 Jan 11. Nat Med. 2016. PMID: 26752518 Free PMC article.
247 results