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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. 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
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: ratcliffe p. 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 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
Low brain penetrant CB1 receptor agonists for the treatment of neuropathic pain.
Adam JM, Clark JK, Davies K, Everett K, Fields R, Francis S, Jeremiah F, Kiyoi T, Maidment M, Morrison A, Ratcliffe P, Prosser A, Schulz J, Wishart G, Baker J, Boyce S, Campbell R, Cottney JE, Deehan M, Martin I. Adam JM, et al. Among authors: ratcliffe p. Bioorg Med Chem Lett. 2012 Apr 15;22(8):2932-7. doi: 10.1016/j.bmcl.2012.02.048. Epub 2012 Feb 23. Bioorg Med Chem Lett. 2012. PMID: 22421020
Rapid access towards follow-up NOP receptor agonists using a knowledge based approach.
Palin R, Clark JK, Evans L, Feilden H, Fletcher D, Hamilton NM, Houghton AK, Jones PS, McArthur D, Montgomery B, Ratcliffe PD, Smith AR, Sutherland A, Weston MA, Wishart G. Palin R, et al. Bioorg Med Chem Lett. 2009 Nov 15;19(22):6441-6. doi: 10.1016/j.bmcl.2009.09.028. Epub 2009 Sep 12. Bioorg Med Chem Lett. 2009. PMID: 19818611
Design, synthesis, and structure-activity relationships of indole-3-heterocycles as agonists of the CB1 receptor.
Morrison AJ, Adam JM, Baker JA, Campbell RA, Clark JK, Cottney JE, Deehan M, Easson AM, Fields R, Francis S, Jeremiah F, Keddie N, Kiyoi T, McArthur DR, Meyer K, Ratcliffe PD, Schulz J, Wishart G, Yoshiizumi K. Morrison AJ, et al. Bioorg Med Chem Lett. 2011 Jan 1;21(1):506-9. doi: 10.1016/j.bmcl.2010.10.093. Epub 2010 Oct 25. Bioorg Med Chem Lett. 2011. PMID: 21075630
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. 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
Imidazopyridyl compounds as aldosterone synthase inhibitors.
Whitehead BR, Lo MM, Ali A, Park MK, Hoyt SB, Xiong Y, Cai J, Carswell E, Cooke A, MacLean J, Ratcliffe P, Robinson J, Bennett DJ, Clemas JA, Wisniewski T, Struthers M, Cully D, MacNeil DJ. Whitehead BR, et al. Among authors: ratcliffe p. Bioorg Med Chem Lett. 2017 Jan 15;27(2):143-146. doi: 10.1016/j.bmcl.2016.12.003. Epub 2016 Dec 2. Bioorg Med Chem Lett. 2017. PMID: 27979595
Fragment-Based Discovery of Novel Potent Sepiapterin Reductase Inhibitors.
Alen J, Schade M, Wagener M, Christian F, Nordhoff S, Merla B, Dunkern TR, Bahrenberg G, Ratcliffe P. Alen J, et al. Among authors: ratcliffe p. J Med Chem. 2019 Jul 11;62(13):6391-6397. doi: 10.1021/acs.jmedchem.9b00218. Epub 2019 Jun 25. J Med Chem. 2019. PMID: 31244106
392 results