| 18342401 |
Catalano A, Carocci A, Corbo F, Franchini C, Muraglia M, Scilimati A, De Bellis M, De Luca A, Camerino DC, Sinicropi MS, Tortorella V: Constrained analogues of tocainide as potent skeletal muscle sodium channel blockers towards the development of antimyotonic agents. Eur J Med Chem. 2008 Nov;43(11):2535-40. Epub 2008 Jan 31.
1-Benzyl-N-(2,6-dimethylphenyl) piperidine-3-carboxamide and 4-benzyl-N-(2,6-dimethylphenyl) piperazine-2-carboxamide, two conformationally restricted analogues of tocainide, were designed and synthesized as voltage-gated skeletal muscle sodium channel blockers. They showed, with respect to tocainide, a marked increase in both potency and use-dependent block. |
32(0,1,1,2) |