| Title | Constrained analogues of tocainide as potent skeletal muscle sodium channel blockers towards the development of antimyotonic agents. | | Author(s) | Catalano A, Carocci A, Corbo F, Franchini C, Muraglia M, Scilimati A, De Bellis M, De Luca A, Camerino DC, Sinicropi MS, Tortorella V | | Institution | Department of Medicinal Chemistry, University of Bari, via E. Orabona n. 4, 70125 Bari, Italy. | | Source | Eur J Med Chem 2008 Jan 31. | | 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. | | Language | ENG | | Pub Type(s) | JOURNAL ARTICLE
| | PubMed ID | 18342401 |
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