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. 2008 Nov;43(11):2535-40.
doi: 10.1016/j.ejmech.2008.01.023. Epub 2008 Jan 31.

Constrained analogues of tocainide as potent skeletal muscle sodium channel blockers towards the development of antimyotonic agents

Alessia Catalano  1 , Alessia Carocci, Filomena Corbo, Carlo Franchini, Marilena Muraglia, Antonio Scilimati, Michela De Bellis, Annamaria De Luca, Diana Conte Camerino, Maria Stefania Sinicropi, Vincenzo Tortorella
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Constrained analogues of tocainide as potent skeletal muscle sodium channel blockers towards the development of antimyotonic agents

Alessia Catalano et al. Eur J Med Chem. 2008 Nov.

Abstract

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.

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