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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: lucas fs. 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 of 2,3-diaryl-pyrazolo[1,5-b]pyridazines as potent and selective cyclooxygenase-2 inhibitors.
Beswick P, Bingham S, Bountra C, Brown T, Browning K, Campbell I, Chessell I, Clayton N, Collins S, Corfield J, Guntrip S, Haslam C, Lambeth P, Lucas F, Mathews N, Murkit G, Naylor A, Pegg N, Pickup E, Player H, Price H, Stevens A, Stratton S, Wiseman J. Beswick P, et al. Bioorg Med Chem Lett. 2004 Nov 1;14(21):5445-8. doi: 10.1016/j.bmcl.2004.07.089. Bioorg Med Chem Lett. 2004. PMID: 15454242
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. 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
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. 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
Pyrazolopyridines as a novel structural class of potent and selective PDE4 inhibitors.
Hamblin JN, Angell TD, Ballantine SP, Cook CM, Cooper AW, Dawson J, Delves CJ, Jones PS, Lindvall M, Lucas FS, Mitchell CJ, Neu MY, Ranshaw LE, Solanke YE, Somers DO, Wiseman JO. Hamblin JN, et al. Among authors: lucas fs. Bioorg Med Chem Lett. 2008 Jul 15;18(14):4237-41. doi: 10.1016/j.bmcl.2008.05.052. Epub 2008 May 17. Bioorg Med Chem Lett. 2008. PMID: 18539455
Quinolines as a novel structural class of potent and selective PDE4 inhibitors: optimisation for oral administration.
Lunniss CJ, Cooper AW, Eldred CD, Kranz M, Lindvall M, Lucas FS, Neu M, Preston AG, Ranshaw LE, Redgrave AJ, Ed Robinson J, Shipley TJ, Solanke YE, Somers DO, Wiseman JO. Lunniss CJ, et al. Among authors: lucas fs. Bioorg Med Chem Lett. 2009 Mar 1;19(5):1380-5. doi: 10.1016/j.bmcl.2009.01.045. Epub 2009 Jan 19. Bioorg Med Chem Lett. 2009. PMID: 19195882
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: lucas fs. 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
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: lucas fs. 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
GSK256066, an exceptionally high-affinity and selective inhibitor of phosphodiesterase 4 suitable for administration by inhalation: in vitro, kinetic, and in vivo characterization.
Tralau-Stewart CJ, Williamson RA, Nials AT, Gascoigne M, Dawson J, Hart GJ, Angell AD, Solanke YE, Lucas FS, Wiseman J, Ward P, Ranshaw LE, Knowles RG. Tralau-Stewart CJ, et al. Among authors: lucas fs. J Pharmacol Exp Ther. 2011 Apr;337(1):145-54. doi: 10.1124/jpet.110.173690. Epub 2011 Jan 4. J Pharmacol Exp Ther. 2011. PMID: 21205923
34 results