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European journal of medicinal chemistry

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


PMID 18342401

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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T0202
Tocainide hydrochloride, ≥98% (HPLC), solid
C11H16N2O · HCl