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Page 1
Structure-activity studies of a novel series of isoxazole-3-carboxamide derivatives as TRPV1 antagonists.
Palin R, Abernethy L, Ansari N, Cameron K, Clarkson T, Dempster M, Dunn D, Easson AM, Edwards D, Maclean J, Everett K, Feilden H, Ho KK, Kultgen S, Littlewood P, McArthur D, McGregor D, McLuskey H, Neagu I, Neale S, Nisbet LA, Ohlmeyer M, Pham Q, Ratcliffe P, Rong Y, Roughton A, Sammons M, Swanson R, Tracey H, Walker G. Palin R, et al. Among authors: edwards d. Bioorg Med Chem Lett. 2011 Feb 1;21(3):892-8. doi: 10.1016/j.bmcl.2010.12.092. Epub 2010 Dec 23. Bioorg Med Chem Lett. 2011. PMID: 21236666
Identification and hit-to-lead optimization of a novel class of CB1 antagonists.
Letourneau JJ, Jokiel P, Olson J, Riviello CM, Ho KK, McAleer L, Yang J, Swanson RN, Baker J, Cowley P, Edwards D, Ward N, Ohlmeyer MH, Webb ML. Letourneau JJ, et al. Among authors: edwards d. Bioorg Med Chem Lett. 2010 Sep 15;20(18):5449-53. doi: 10.1016/j.bmcl.2010.07.091. Epub 2010 Jul 25. Bioorg Med Chem Lett. 2010. PMID: 20719511
The discovery of novel indole-2-carboxamides as cannabinoid CB(1) receptor antagonists.
Cowley PM, Baker J, Barn DR, Buchanan KI, Carlyle I, Clark JK, Clarkson TR, Deehan M, Edwards D, Goodwin RR, Jaap D, Kiyoi Y, Mort C, Palin R, Prosser A, Walker G, Ward N, Wishart G, Young T. Cowley PM, et al. Among authors: edwards d. Bioorg Med Chem Lett. 2011 Jan 1;21(1):497-501. doi: 10.1016/j.bmcl.2010.10.104. Epub 2010 Oct 26. Bioorg Med Chem Lett. 2011. PMID: 21075628
Discovery of potent and orally bioavailable heterocycle-based cannabinoid CB1 receptor agonists.
Kiyoi T, Adam JM, Clark JK, Davies K, Easson AM, Edwards D, Feilden H, Fields R, Francis S, Jeremiah F, McArthur D, Morrison AJ, Prosser A, Ratcliffe PD, Schulz J, Wishart G, Baker J, Campbell R, Cottney JE, Deehan M, Epemolu O, Evans L. Kiyoi T, et al. Among authors: edwards d. Bioorg Med Chem Lett. 2011 Mar 15;21(6):1748-53. doi: 10.1016/j.bmcl.2011.01.082. Epub 2011 Jan 22. Bioorg Med Chem Lett. 2011. PMID: 21316962
Pharmacokinetic optimisation of novel indole-2-carboxamide cannabinoid CB1 antagonists.
Cowley PM, Baker J, Buchanan KI, Carlyle I, Clark JK, Clarkson TR, Deehan M, Edwards D, Kiyoi Y, Martin I, Osbourn D, Walker G, Ward N, Wishart G. Cowley PM, et al. Among authors: edwards d. Bioorg Med Chem Lett. 2011 Apr 1;21(7):2034-9. doi: 10.1016/j.bmcl.2011.02.019. Epub 2011 Feb 19. Bioorg Med Chem Lett. 2011. PMID: 21334892
Design, synthesis and structure-activity relationships of (indo-3-yl) heterocyclic derivatives as agonists of the CB1 receptor. Discovery of a clinical candidate.
Ratcliffe P, Adam JM, Baker J, Bursi R, Campbell R, Clark JK, Cottney JE, Deehan M, Easson AM, Ecker D, Edwards D, Epemolu O, Evans L, Fields R, Francis S, Harradine P, Jeremiah F, Kiyoi T, McArthur D, Morrison A, Passier P, Pick J, Schnabel PG, Schulz J, Steinbrede H, Walker G, Westwood P, Wishart G, Udo de Haes J. Ratcliffe P, et al. Among authors: edwards d. Bioorg Med Chem Lett. 2011 Apr 15;21(8):2541-6. doi: 10.1016/j.bmcl.2011.02.023. Epub 2011 Feb 12. Bioorg Med Chem Lett. 2011. PMID: 21411321
Identification of potent, soluble, and orally active TRPV1 antagonists.
Ratcliffe P, Maclean J, Abernethy L, Clarkson T, Dempster M, Easson AM, Edwards D, Everett K, Feilden H, Littlewood P, McArthur D, McGregor D, McLuskey H, Nimz O, Nisbet LA, Palin R, Tracey H, Walker G. Ratcliffe P, et al. Among authors: edwards d. Bioorg Med Chem Lett. 2011 Apr 15;21(8):2559-63. doi: 10.1016/j.bmcl.2011.01.112. Epub 2011 Jan 31. Bioorg Med Chem Lett. 2011. PMID: 21435873
Discovery of potent, soluble and orally active TRPV1 antagonists. Structure-activity relationships of a series of isoxazoles.
Ratcliffe P, Abernethy L, Ansari N, Cameron K, Clarkson T, Dempster M, Dunn D, Easson AM, Edwards D, Everett K, Feilden H, Ho KK, Kultgen S, Littlewood P, Maclean J, McArthur D, McGregor D, McLuskey H, Neagu I, Nimz O, Nisbet LA, Ohlmeyer M, Palin R, Pham Q, Rong Y, Roughton A, Sammons M, Swanson R, Tracey H, Walker G. Ratcliffe P, et al. Among authors: edwards d. Bioorg Med Chem Lett. 2011 Aug 1;21(15):4652-7. doi: 10.1016/j.bmcl.2011.01.051. Epub 2011 Jan 26. Bioorg Med Chem Lett. 2011. PMID: 21723725
Structure-Guided Design and Synthesis of a Pyridazinone Series of Trypanosoma cruzi Proteasome Inhibitors.
Thomas MG, McGonagle K, Rowland P, Robinson DA, Dodd PG, Camino-Díaz I, Campbell L, Cantizani J, Castañeda P, Conn D, Craggs PD, Edwards D, Ferguson L, Fosberry A, Frame L, Goswami P, Hu X, Korczynska J, MacLean L, Martin J, Mutter N, Osuna-Cabello M, Paterson C, Peña I, Pinto EG, Pont C, Riley J, Shishikura Y, Simeons FRC, Stojanovski L, Thomas J, Wrobel K, Young RJ, Zmuda F, Zuccotto F, Read KD, Gilbert IH, Marco M, Miles TJ, Manzano P, De Rycker M. Thomas MG, et al. Among authors: edwards d. J Med Chem. 2023 Aug 10;66(15):10413-10431. doi: 10.1021/acs.jmedchem.3c00582. Epub 2023 Jul 28. J Med Chem. 2023. PMID: 37506194 Free PMC article.
3,787 results