Constrained analogues of tocainide as potent skeletal muscle sodium channel blockers towards the development of antimyotonic agents.
نویسندگان
چکیده
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.
منابع مشابه
Increased sodium channel use-dependent inhibition by a new potent analogue of tocainide greatly enhances in vivo antimyotonic activity
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عنوان ژورنال:
- European journal of medicinal chemistry
دوره 43 11 شماره
صفحات -
تاریخ انتشار 2008