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.
Constrained analogues of tocainide as potent skeletal muscle sodium channel blockers towards the development of antimyotonic agents
CATALANO, ALESSIA;CAROCCI, ALESSIA;CORBO, Filomena Faustina Rina;FRANCHINI, Carlo;MURAGLIA M;SCILIMATI, Antonio;DE BELLIS, MICHELA;DE LUCA, Annamaria;CONTE, Diana;TORTORELLA, Vincenzo
2008-01-01
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.File in questo prodotto:
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