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Discovery of a Potent, Selective T-type Calcium Channel Blocker as a Drug Candidate for the Treatment of Generalized Epilepsies.
Bezençon O, Heidmann B, Siegrist R, Stamm S, Richard S, Pozzi D, Corminboeuf O, Roch C, Kessler M, Ertel EA, Reymond I, Pfeifer T, de Kanter R, Toeroek-Schafroth M, Moccia LG, Mawet J, Moon R, Rey M, Capeleto B, Fournier E. Bezençon O, et al. Among authors: moccia lg. J Med Chem. 2017 Dec 14;60(23):9769-9789. doi: 10.1021/acs.jmedchem.7b01236. Epub 2017 Nov 20. J Med Chem. 2017. PMID: 29116786
Milestones to the Discovery of T-type Calcium Channel Blockers for the Treatment of Generalized Epilepsies.
Bezençon O, Siegrist R, Heidmann B, Pozzi D, Stamm S, Remeň L, Richard S, Simons L, Gaston R, Downing D, Grisostomi C, Roch C, Kessler M, Gatfield J, Moon R, Pfeifer T, Mosbacher J, Reymond I, Ertel EA, de Kanter R, Capeleto B, Fournier E, Rey M, Moccia L, Toeroek-Schafroth M, Roscher R, Schindelholz B. Bezençon O, et al. Chimia (Aarau). 2017 Oct 25;71(10):722-729. doi: 10.2533/chimia.2017.722. Chimia (Aarau). 2017. PMID: 29070417 Free article.
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