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Page 1
BACE-1 inhibitors part 1: identification of novel hydroxy ethylamines (HEAs).
Clarke B, Demont E, Dingwall C, Dunsdon R, Faller A, Hawkins J, Hussain I, MacPherson D, Maile G, Matico R, Milner P, Mosley J, Naylor A, O'Brien A, Redshaw S, Riddell D, Rowland P, Soleil V, Smith KJ, Stanway S, Stemp G, Sweitzer S, Theobald P, Vesey D, Walter DS, Ward J, Wayne G. Clarke B, et al. Among authors: theobald p. Bioorg Med Chem Lett. 2008 Feb 1;18(3):1011-6. doi: 10.1016/j.bmcl.2007.12.017. Epub 2007 Dec 15. Bioorg Med Chem Lett. 2008. PMID: 18171614
BACE-1 inhibitors part 2: identification of hydroxy ethylamines (HEAs) with reduced peptidic character.
Clarke B, Demont E, Dingwall C, Dunsdon R, Faller A, Hawkins J, Hussain I, MacPherson D, Maile G, Matico R, Milner P, Mosley J, Naylor A, O'Brien A, Redshaw S, Riddell D, Rowland P, Soleil V, Smith KJ, Stanway S, Stemp G, Sweitzer S, Theobald P, Vesey D, Walter DS, Ward J, Wayne G. Clarke B, et al. Among authors: theobald p. Bioorg Med Chem Lett. 2008 Feb 1;18(3):1017-21. doi: 10.1016/j.bmcl.2007.12.019. Epub 2007 Dec 15. Bioorg Med Chem Lett. 2008. PMID: 18166458
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. Among authors: theobald p. 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
Second generation of hydroxyethylamine BACE-1 inhibitors: optimizing potency and oral bioavailability.
Charrier N, Clarke B, Cutler L, Demont E, Dingwall C, Dunsdon R, East P, Hawkins J, Howes C, Hussain I, Jeffrey P, Maile G, Matico R, Mosley J, Naylor A, O'Brien A, Redshaw S, Rowland P, Soleil V, Smith KJ, Sweitzer S, Theobald P, Vesey D, Walter DS, Wayne G. Charrier N, et al. Among authors: theobald p. J Med Chem. 2008 Jun 12;51(11):3313-7. doi: 10.1021/jm800138h. Epub 2008 May 6. J Med Chem. 2008. PMID: 18457381
Second generation of BACE-1 inhibitors part 3: Towards non hydroxyethylamine transition state mimetics.
Charrier N, Clarke B, Cutler L, Demont E, Dingwall C, Dunsdon R, Hawkins J, Howes C, Hubbard J, Hussain I, Maile G, Matico R, Mosley J, Naylor A, O'Brien A, Redshaw S, Rowland P, Soleil V, Smith KJ, Sweitzer S, Theobald P, Vesey D, Walter DS, Wayne G. Charrier N, et al. Among authors: theobald p. Bioorg Med Chem Lett. 2009 Jul 1;19(13):3674-8. doi: 10.1016/j.bmcl.2009.03.149. Epub 2009 Apr 5. Bioorg Med Chem Lett. 2009. PMID: 19406640
Second generation of BACE-1 inhibitors. Part 1: The need for improved pharmacokinetics.
Charrier N, Clarke B, Cutler L, Demont E, Dingwall C, Dunsdon R, Hawkins J, Howes C, Hubbard J, Hussain I, Maile G, Matico R, Mosley J, Naylor A, O'Brien A, Redshaw S, Rowland P, Soleil V, Smith KJ, Sweitzer S, Theobald P, Vesey D, Walter DS, Wayne G. Charrier N, et al. Among authors: theobald p. Bioorg Med Chem Lett. 2009 Jul 1;19(13):3664-8. doi: 10.1016/j.bmcl.2009.03.165. Epub 2009 Apr 17. Bioorg Med Chem Lett. 2009. PMID: 19428244
Second generation of BACE-1 inhibitors part 2: Optimisation of the non-prime side substituent.
Charrier N, Clarke B, Demont E, Dingwall C, Dunsdon R, Hawkins J, Hubbard J, Hussain I, Maile G, Matico R, Mosley J, Naylor A, O'Brien A, Redshaw S, Rowland P, Soleil V, Smith KJ, Sweitzer S, Theobald P, Vesey D, Walter DS, Wayne G. Charrier N, et al. Among authors: theobald p. Bioorg Med Chem Lett. 2009 Jul 1;19(13):3669-73. doi: 10.1016/j.bmcl.2009.03.150. Epub 2009 Apr 5. Bioorg Med Chem Lett. 2009. PMID: 19477642
BACE-1 hydroxyethylamine inhibitors using novel edge-to-face interaction with Arg-296.
Clarke B, Cutler L, Demont E, Dingwall C, Dunsdon R, Hawkins J, Howes C, Hussain I, Maile G, Matico R, Mosley J, Naylor A, O'Brien A, Redshaw S, Rowland P, Soleil V, Smith KJ, Sweitzer S, Theobald P, Vesey D, Walter DS, Wayne G. Clarke B, et al. Among authors: theobald p. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4639-44. doi: 10.1016/j.bmcl.2010.05.111. Epub 2010 Jun 8. Bioorg Med Chem Lett. 2010. PMID: 20579874
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: theobald pj. 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
Identification of a series of 1,3,4-oxadiazol-2-amines as potent alpha-7 agonists with efficacy in the novel object recognition model of cognition.
Skidmore J, Atcha Z, Boucherat E, Castelletti L, Chen DW, Coppo FT, Cutler L, Dunsdon RM, Heath BM, Hutchings R, Hurst DN, Javed S, Martin S, Maskell ES, Norton D, Pemberton DJ, Redshaw S, Rutter R, Sehmi SS, Scoccitti T, Temple HE, Theobald P, Ward RW, Wilson DM. Skidmore J, et al. Among authors: theobald p. Bioorg Med Chem Lett. 2012 May 15;22(10):3560-3. doi: 10.1016/j.bmcl.2012.03.040. Epub 2012 Mar 16. Bioorg Med Chem Lett. 2012. PMID: 22503248
98 results