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Page 1
Identification of [4-[4-(methylsulfonyl)phenyl]-6-(trifluoromethyl)-2-pyrimidinyl] amines and ethers as potent and selective cyclooxygenase-2 inhibitors.
Swarbrick ME, Beswick PJ, Gleave RJ, Green RH, Bingham S, Bountra C, Carter MC, Chambers LJ, Chessell IP, Clayton NM, Collins SD, Corfield JA, Hartley CD, Kleanthous S, Lambeth PF, Lucas FS, Mathews N, Naylor A, Page LW, Payne JJ, Pegg NA, Price HS, Skidmore J, Stevens AJ, Stocker R, Stratton SC, Stuart AJ, Wiseman JO. Swarbrick ME, et al. Among authors: gleave rj. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4504-8. doi: 10.1016/j.bmcl.2009.02.085. Epub 2009 Feb 26. Bioorg Med Chem Lett. 2009. PMID: 19520573
Identification and optimisation of a novel series of pyrimidine based cyclooxygenase-2 (COX-2) inhibitors. Utilisation of a biotransformation approach.
Beswick PJ, Blackaby AP, Bountra C, Brown T, Browning K, Campbell IB, Corfield J, Gleave RJ, Guntrip SB, Hall RM, Hindley S, Lambeth PF, Lucas F, Mathews N, Naylor A, Player H, Price HS, Sidebottom PJ, Taylor NL, Webb G, Wiseman J. Beswick PJ, et al. Among authors: gleave rj. Bioorg Med Chem Lett. 2009 Aug 1;19(15):4509-14. doi: 10.1016/j.bmcl.2009.02.089. Epub 2009 Feb 27. Bioorg Med Chem Lett. 2009. PMID: 19523822
Synthesis and structure-activity relationships of a series of (1H-pyrazol-4-yl)acetamide antagonists of the P2X7 receptor.
Chambers LJ, Stevens AJ, Moses AP, Michel AD, Walter DS, Davies DJ, Livermore DG, Fonfria E, Demont EH, Vimal M, Theobald PJ, Beswick PJ, Gleave RJ, Roman SA, Senger S. Chambers LJ, et al. Among authors: gleave rj. Bioorg Med Chem Lett. 2010 May 15;20(10):3161-4. doi: 10.1016/j.bmcl.2010.03.096. Epub 2010 Mar 30. Bioorg Med Chem Lett. 2010. PMID: 20399651
Structure-activity relationships and in vivo activity of (1H-pyrazol-4-yl)acetamide antagonists of the P2X(7) receptor.
Beswick PJ, Billinton A, Chambers LJ, Dean DK, Fonfria E, Gleave RJ, Medhurst SJ, Michel AD, Moses AP, Patel S, Roman SA, Roomans S, Senger S, Stevens AJ, Walter DS. Beswick PJ, et al. Among authors: gleave rj. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4653-6. doi: 10.1016/j.bmcl.2010.05.107. Epub 2010 Jun 8. Bioorg Med Chem Lett. 2010. PMID: 20579878
Discovery and structure-activity relationships of a series of pyroglutamic acid amide antagonists of the P2X7 receptor.
Abdi MH, Beswick PJ, Billinton A, Chambers LJ, Charlton A, Collins SD, Collis KL, Dean DK, Fonfria E, Gleave RJ, Lejeune CL, Livermore DG, Medhurst SJ, Michel AD, Moses AP, Page L, Patel S, Roman SA, Senger S, Slingsby B, Steadman JG, Stevens AJ, Walter DS. Abdi MH, et al. Among authors: gleave rj. Bioorg Med Chem Lett. 2010 Sep 1;20(17):5080-4. doi: 10.1016/j.bmcl.2010.07.033. Epub 2010 Jul 14. Bioorg Med Chem Lett. 2010. PMID: 20673717
BACE-1 inhibitors part 3: identification of hydroxy ethylamines (HEAs) with nanomolar potency in cells.
Beswick P, Charrier N, Clarke B, Demont E, Dingwall C, Dunsdon R, Faller A, Gleave R, Hawkins J, Hussain I, Johnson CN, MacPherson D, Maile G, Matico R, Milner P, Mosley J, Naylor A, O'Brien A, Redshaw S, Riddell D, Rowland P, Skidmore J, Soleil V, Smith KJ, Stanway S, Stemp G, Stuart A, Sweitzer S, Theobald P, Vesey D, Walter DS, Ward J, Wayne G. Beswick P, et al. Bioorg Med Chem Lett. 2008 Feb 1;18(3):1022-6. doi: 10.1016/j.bmcl.2007.12.020. Epub 2007 Dec 15. Bioorg Med Chem Lett. 2008. PMID: 18171615
Structure-activity relationships of 1,5-biaryl pyrroles as EP1 receptor antagonists.
Hall A, Atkinson S, Brown SH, Chessell IP, Chowdhury A, Clayton NM, Coleman T, Giblin GM, Gleave RJ, Hammond B, Healy MP, Johnson MR, Michel AD, Naylor A, Novelli R, Spalding DJ, Tang SP. Hall A, et al. Among authors: gleave rj. Bioorg Med Chem Lett. 2006 Jul 15;16(14):3657-62. doi: 10.1016/j.bmcl.2006.04.073. Epub 2006 May 11. Bioorg Med Chem Lett. 2006. PMID: 16697196
14 results