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Page 1
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: murkitt g. 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
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: murkitt g. 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
New quinoline NK3 receptor antagonists with CNS activity.
Smith PW, Wyman PA, Lovell P, Goodacre C, Serafinowska HT, Vong A, Harrington F, Flynn S, Bradley DM, Porter R, Coggon S, Murkitt G, Searle K, Thomas DR, Watson JM, Martin W, Wu Z, Dawson LA. Smith PW, et al. Among authors: murkitt g. Bioorg Med Chem Lett. 2009 Feb 1;19(3):837-40. doi: 10.1016/j.bmcl.2008.12.005. Epub 2008 Dec 7. Bioorg Med Chem Lett. 2009. PMID: 19117759
The discovery of a series of N-substituted 3-(4-piperidinyl)-1,3-benzoxazolinones and oxindoles as highly brain penetrant, selective muscarinic M1 agonists.
Johnson DJ, Forbes IT, Watson SP, Garzya V, Stevenson GI, Walker GR, Mudhar HS, Flynn ST, Wyman PA, Smith PW, Murkitt GS, Lucas AJ, Mookherjee CR, Watson JM, Gartlon JE, Bradford AM, Brown F. Johnson DJ, et al. Among authors: murkitt gs. Bioorg Med Chem Lett. 2010 Sep 15;20(18):5434-8. doi: 10.1016/j.bmcl.2010.07.097. Epub 2010 Jul 30. Bioorg Med Chem Lett. 2010. PMID: 20709550
In vitro and in vivo comparison of two non-peptide tachykinin NK3 receptor antagonists: Improvements in efficacy achieved through enhanced brain penetration or altered pharmacological characteristics.
Dawson LA, Langmead CJ, Dada A, Watson JM, Wu Z, de la Flor R, Jones GA, Cluderay JE, Southam E, Murkitt GS, Hill MD, Jones DN, Davies CH, Hagan JJ, Smith PW. Dawson LA, et al. Among authors: murkitt gs. Eur J Pharmacol. 2010 Feb 10;627(1-3):106-14. doi: 10.1016/j.ejphar.2009.10.054. Epub 2009 Oct 30. Eur J Pharmacol. 2010. PMID: 19879867
In vitro and in vivo characterization of the non-peptide NK3 receptor antagonist SB-223412 (talnetant): potential therapeutic utility in the treatment of schizophrenia.
Dawson LA, Cato KJ, Scott C, Watson JM, Wood MD, Foxton R, de la Flor R, Jones GA, Kew JN, Cluderay JE, Southam E, Murkitt GS, Gartlon J, Pemberton DJ, Jones DN, Davies CH, Hagan J. Dawson LA, et al. Among authors: murkitt gs. Neuropsychopharmacology. 2008 Jun;33(7):1642-52. doi: 10.1038/sj.npp.1301549. Epub 2007 Aug 29. Neuropsychopharmacology. 2008. PMID: 17728699
The cyclooxygenase-2 inhibitor GW406381X [2-(4-ethoxyphenyl)-3-[4-(methylsulfonyl)phenyl]-pyrazolo[1,5-b]pyridazine] is effective in animal models of neuropathic pain and central sensitization.
Bingham S, Beswick PJ, Bountra C, Brown T, Campbell IB, Chessell IP, Clayton N, Collins SD, Davey PT, Goodland H, Gray N, Haslam C, Hatcher JP, Hunter AJ, Lucas F, Murkitt G, Naylor A, Pickup E, Sargent B, Summerfield SG, Stevens A, Stratton SC, Wiseman J. Bingham S, et al. Among authors: murkitt g. J Pharmacol Exp Ther. 2005 Mar;312(3):1161-9. doi: 10.1124/jpet.104.075267. Epub 2004 Nov 30. J Pharmacol Exp Ther. 2005. PMID: 15572651
16 results