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Page 1
Design and synthesis of trans-3-(2-(4-((3-(3-(5-methyl-1,2,4-oxadiazolyl))- phenyl)carboxamido)cyclohexyl)ethyl)-7-methylsulfonyl-2,3,4,5-tetrahydro-1H-3-benzazepine (SB-414796): a potent and selective dopamine D3 receptor antagonist.
Macdonald GJ, Branch CL, Hadley MS, Johnson CN, Nash DJ, Smith AB, Stemp G, Thewlis KM, Vong AK, Austin NE, Jeffrey P, Winborn KY, Boyfield I, Hagan JJ, Middlemiss DN, Reavill C, Riley GJ, Watson JM, Wood M, Parker SG, Ashby CR Jr. Macdonald GJ, et al. Among authors: thewlis km. J Med Chem. 2003 Nov 6;46(23):4952-64. doi: 10.1021/jm030817d. J Med Chem. 2003. PMID: 14584946
3,4-Dihydro-2H-benzoxazinones are 5-HT(1A) receptor antagonists with potent 5-HT reuptake inhibitory activity.
Atkinson PJ, Bromidge SM, Duxon MS, Gaster LM, Hadley MS, Hammond B, Johnson CN, Middlemiss DN, North SE, Price GW, Rami HK, Riley GJ, Scott CM, Shaw TE, Starr KR, Stemp G, Thewlis KM, Thomas DR, Thompson M, Vong AK, Watson JM. Atkinson PJ, et al. Among authors: thewlis km. Bioorg Med Chem Lett. 2005 Feb 1;15(3):737-41. doi: 10.1016/j.bmcl.2004.11.030. Bioorg Med Chem Lett. 2005. PMID: 15664848
Studies on a series of potent, orally bioavailable, 5-HT(1) receptor ligands.
Ward SE, Johnson CN, Lovell PJ, Scott CM, Smith PW, Stemp G, Thewlis KM, Vong AK, Watson JM. Ward SE, et al. Among authors: thewlis km. Bioorg Med Chem Lett. 2007 Sep 15;17(18):5214-7. doi: 10.1016/j.bmcl.2007.06.078. Epub 2007 Jun 30. Bioorg Med Chem Lett. 2007. PMID: 17629698
Discovery of N-[(2S)-5-(6-fluoro-3-pyridinyl)-2,3-dihydro-1H-inden-2-yl]-2-propanesulfonamide, a novel clinical AMPA receptor positive modulator.
Ward SE, Harries M, Aldegheri L, Andreotti D, Ballantine S, Bax BD, Harris AJ, Harker AJ, Lund J, Melarange R, Mingardi A, Mookherjee C, Mosley J, Neve M, Oliosi B, Profeta R, Smith KJ, Smith PW, Spada S, Thewlis KM, Yusaf SP. Ward SE, et al. Among authors: thewlis km. J Med Chem. 2010 Aug 12;53(15):5801-12. doi: 10.1021/jm1005429. J Med Chem. 2010. PMID: 20614889 Clinical Trial.
Integration of lead optimization with crystallography for a membrane-bound ion channel target: discovery of a new class of AMPA receptor positive allosteric modulators.
Ward SE, Harries M, Aldegheri L, Austin NE, Ballantine S, Ballini E, Bradley DM, Bax BD, Clarke BP, Harris AJ, Harrison SA, Melarange RA, Mookherjee C, Mosley J, Dal Negro G, Oliosi B, Smith KJ, Thewlis KM, Woollard PM, Yusaf SP. Ward SE, et al. Among authors: thewlis km. J Med Chem. 2011 Jan 13;54(1):78-94. doi: 10.1021/jm100679e. Epub 2010 Dec 3. J Med Chem. 2011. PMID: 21128618
Model studies on a synthetically facile series of N-substituted phenyl-N'-pyridin-3-yl ureas leading to 1-(3-pyridylcarbamoyl) indolines that are potent and selective 5-HT(2C/2B) receptor antagonists.
Bromidge SM, Dabbs S, Davies DT, Davies S, Duckworth DM, Forbes IT, Gadre A, Ham P, Jones GE, King FD, Saunders DV, Thewlis KM, Vyas D, Blackburn TP, Holland V, Kennett GA, Riley GJ, Wood MD. Bromidge SM, et al. Among authors: thewlis km. Bioorg Med Chem. 1999 Dec;7(12):2767-73. doi: 10.1016/s0968-0896(99)00228-x. Bioorg Med Chem. 1999. PMID: 10658582
22 results