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Page 1
Synthesis and SAR of novel GPR39 agonists and positive allosteric modulators.
Burley R, Hewer RC, Teall M, Dickson L, Ossola B, Russell S, Bender C, Cheung T, Powell JAC, Xu X, Brice NL, Otter L, Arimont M, Kidd SL, Vidal D, Dale JW, Mervin L, Sore HF, Mateu N, Lakshminarayana N, Dawson LA, Carlton M, Bürli RW. Burley R, et al. Among authors: dawson la. Bioorg Med Chem Lett. 2022 Apr 1;61:128607. doi: 10.1016/j.bmcl.2022.128607. Epub 2022 Feb 3. Bioorg Med Chem Lett. 2022. PMID: 35123006
Development of CVN424: A Selective and Novel GPR6 Inverse Agonist Effective in Models of Parkinson Disease.
Brice NL, Schiffer HH, Monenschein H, Mulligan VJ, Page K, Powell J, Xu X, Cheung T, Burley JR, Sun H, Dickson L, Murphy ST, Kaushal N, Sheardown S, Lawrence J, Chen Y, Bartkowski D, Kanta A, Russo J, Hosea N, Dawson LA, Hitchcock SH, Carlton MB. Brice NL, et al. Among authors: dawson la. J Pharmacol Exp Ther. 2021 Jun;377(3):407-416. doi: 10.1124/jpet.120.000438. Epub 2021 Apr 1. J Pharmacol Exp Ther. 2021. PMID: 33795395
Identification and optimisation of a series of tetrahydrobenzotriazoles as metabotropic glutamate receptor 5-selective positive allosteric modulators that improve performance in a preclinical model of cognition.
Ellard JM, Madin A, Philps O, Hopkin M, Henderson S, Birch L, O'Connor D, Arai T, Takase K, Morgan L, Reynolds D, Talma S, Howley E, Powney B, Payne AH, Hall A, Gartlon JE, Dawson LA, Castro L, Atkinson PJ. Ellard JM, et al. Among authors: dawson la. Bioorg Med Chem Lett. 2015 Dec 15;25(24):5792-6. doi: 10.1016/j.bmcl.2015.10.050. Epub 2015 Oct 17. Bioorg Med Chem Lett. 2015. PMID: 26531152
Identification of a potent and selective 5-HT1B receptor antagonist.
Wyman PA, Marshall HR, Flynn ST, King RJ, Thompson M, Smith PW, Hadley MS, Price GW, Scott CM, Dawson LA. Wyman PA, et al. Among authors: dawson la. Bioorg Med Chem Lett. 2005 Nov 1;15(21):4708-12. doi: 10.1016/j.bmcl.2005.07.085. Bioorg Med Chem Lett. 2005. PMID: 16153839
Discovery of N1-(6-chloroimidazo[2,1-b][1,3]thiazole-5-sulfonyl)tryptamine as a potent, selective, and orally active 5-HT(6) receptor agonist.
Cole DC, Stock JR, Lennox WJ, Bernotas RC, Ellingboe JW, Boikess S, Coupet J, Smith DL, Leung L, Zhang GM, Feng X, Kelly MF, Galante R, Huang P, Dawson LA, Marquis K, Rosenzweig-Lipson S, Beyer CE, Schechter LE. Cole DC, et al. Among authors: dawson la. J Med Chem. 2007 Nov 15;50(23):5535-8. doi: 10.1021/jm070521y. Epub 2007 Oct 19. J Med Chem. 2007. PMID: 17948978
New quinoline NK3 receptor antagonists with CNS activity.
Smith PW, Wyman PA, Lovell P, Goodacre C, Serafinowska HT, Vong A, Harrington F, Flynn S, Bradley DM, Porter R, Coggon S, Murkitt G, Searle K, Thomas DR, Watson JM, Martin W, Wu Z, Dawson LA. Smith PW, et al. Among authors: dawson la. Bioorg Med Chem Lett. 2009 Feb 1;19(3):837-40. doi: 10.1016/j.bmcl.2008.12.005. Epub 2008 Dec 7. Bioorg Med Chem Lett. 2009. PMID: 19117759
Fragment-Based Discovery of a Novel, Brain Penetrant, Orally Active HDAC2 Inhibitor.
Tamanini E, Miyamura S, Buck IM, Cons BD, Dawson L, East C, Futamura T, Goto S, Griffiths-Jones C, Hashimoto T, Heightman TD, Ishikawa S, Ito H, Kaneko Y, Kawato T, Kondo K, Kurihara N, McCarthy JM, Mori Y, Nagase T, Nakaishi Y, Reeks J, Sato A, Schöpf P, Tai K, Tamai T, Tisi D, Woolford AJ. Tamanini E, et al. ACS Med Chem Lett. 2022 Sep 6;13(10):1591-1597. doi: 10.1021/acsmedchemlett.2c00272. eCollection 2022 Oct 13. ACS Med Chem Lett. 2022. PMID: 36262388 Free PMC article.
Pharmacological characterization of N-[(2S)-5-(6-fluoro-3-pyridinyl)-2, 3-dihydro-1H-inden-2-yl]-2-propanesulfonamide: a novel, clinical AMPA receptor positive allosteric modulator.
Ward SE, Beswick P, Calcinaghi N, Dawson LA, Gartlon J, Graziani F, Jones DN, Lacroix L, Selina Mok MH, Oliosi B, Pardoe J, Starr K, Woolley ML, Harries MH. Ward SE, et al. Among authors: dawson la. Br J Pharmacol. 2017 Mar;174(5):370-385. doi: 10.1111/bph.13696. Epub 2017 Jan 31. Br J Pharmacol. 2017. PMID: 28009436 Free PMC article.
385 results