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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: bromidge sm. 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
Design and synthesis of novel tricyclic benzoxazines as potent 5-HT(1A/B/D) receptor antagonists leading to the discovery of 6-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-4H-imidazo[5,1-c][1,4]benzoxazine-3-carboxamide (GSK588045).
Bromidge SM, Arban R, Bertani B, Bison S, Borriello M, Cavanni P, Dal Forno G, Di-Fabio R, Donati D, Fontana S, Gianotti M, Gordon LJ, Granci E, Leslie CP, Moccia L, Pasquarello A, Sartori I, Sava A, Watson JM, Worby A, Zonzini L, Zucchelli V. Bromidge SM, et al. J Med Chem. 2010 Aug 12;53(15):5827-43. doi: 10.1021/jm100482n. J Med Chem. 2010. PMID: 20590088
5-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}-2(1H)-quinolinones and 3,4-dihydro-2(1H)-quinolinones: dual-acting 5-HT1 receptor antagonists and serotonin reuptake inhibitors. Part 3.
Bromidge SM, Arban R, Bertani B, Borriello M, Capelli AM, Di-Fabio R, Faedo S, Gianotti M, Gordon LJ, Granci E, Pasquarello A, Spada SK, Worby A, Zonzini L, Zucchelli V. Bromidge SM, et al. Bioorg Med Chem Lett. 2010 Dec 1;20(23):7092-6. doi: 10.1016/j.bmcl.2010.09.085. Epub 2010 Sep 27. Bioorg Med Chem Lett. 2010. PMID: 20951584
Bicyclic heteroarylpiperazines as selective brain penetrant 5-HT6 receptor antagonists.
Ahmed M, Briggs MA, Bromidge SM, Buck T, Campbell L, Deeks NJ, Garner A, Gordon L, Hamprecht DW, Holland V, Johnson CN, Medhurst AD, Mitchell DJ, Moss SF, Powles J, Seal JT, Stean TO, Stemp G, Thompson M, Trail B, Upton N, Winborn K, Witty DR. Ahmed M, et al. Among authors: bromidge sm. Bioorg Med Chem Lett. 2005 Nov 1;15(21):4867-71. doi: 10.1016/j.bmcl.2005.06.107. Bioorg Med Chem Lett. 2005. PMID: 16143522
Discovery of 1-(3-{2-[4-(2-methyl-5-quinolinyl)-1-piperazinyl]ethyl}phenyl)-2-imidazolidinone (GSK163090), a Potent, selective, and orally active 5-HT1A/B/D receptor antagonist.
Leslie CP, Biagetti M, Bison S, Bromidge SM, Di Fabio R, Donati D, Falchi A, Garnier MJ, Jaxa-Chamiec A, Manchee G, Merlo G, Pizzi DA, Stasi LP, Tibasco J, Vong A, Ward SE, Zonzini L. Leslie CP, et al. Among authors: bromidge sm. J Med Chem. 2010 Dec 9;53(23):8228-40. doi: 10.1021/jm100714c. Epub 2010 Nov 5. J Med Chem. 2010. PMID: 21053897
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