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Page 1
Discovery of Benzimidazole CYP11B2 Inhibitors with in Vivo Activity in Rhesus Monkeys.
Hoyt SB, Park MK, London C, Xiong Y, Tata J, Bennett DJ, Cooke A, Cai J, Carswell E, Robinson J, MacLean J, Brown L, Belshaw S, Clarkson TR, Liu K, Liang GB, Struthers M, Cully D, Wisniewski T, Ren N, Bopp C, Sok A, Cai TQ, Stribling S, Pai LY, Ma X, Metzger J, Verras A, McMasters D, Chen Q, Tung E, Tang W, Salituro G, Buist N, Kuethe J, Rivera N, Clemas J, Zhou G, Gibson J, Maxwell CA, Lassman M, McLaughlin T, Castro-Perez J, Szeto D, Forrest G, Hajdu R, Rosenbach M, Ali A. Hoyt SB, et al. Among authors: clarkson tr. ACS Med Chem Lett. 2015 Apr 7;6(5):573-8. doi: 10.1021/acsmedchemlett.5b00054. eCollection 2015 May 14. ACS Med Chem Lett. 2015. PMID: 26005536 Free PMC article.
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. 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. 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-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. 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
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: clarkson tr. 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
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: clarkson tr. 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
The discovery and SAR of indoline-3-carboxamides--a new series of 5-HT6 antagonists.
Reid M, Carlyle I, Caulfield WL, Clarkson TR, Cusick F, Epemolu O, Gilfillan R, Goodwin R, Jaap D, O'Donnell EC, Presland J, Rankovic Z, Spinks D, Spinks G, Thomson AM, Thomson F, Strain J, Wishart G. Reid M, et al. Among authors: clarkson tr. Bioorg Med Chem Lett. 2010 Jun 15;20(12):3713-6. doi: 10.1016/j.bmcl.2010.04.085. Epub 2010 Apr 24. Bioorg Med Chem Lett. 2010. PMID: 20471831