title: Constrained analogues of tocainide as potent skeletal muscle sodium channel blockers towards the development of antimyotonic agents.
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.
authors.affiliation: Department of Medicinal Chemistry, University of Bari, via E. Orabona n. 4, 70125 Bari, Italy.
authors.forename: Alessia
authors.initials: A
authors.lastname: Catalano
authors.forename: Alessia
authors.initials: A
authors.lastname: Carocci
authors.forename: Filomena
authors.initials: F
authors.lastname: Corbo
authors.forename: Carlo
authors.initials: C
authors.lastname: Franchini
authors.forename: Marilena
authors.initials: M
authors.lastname: Muraglia
authors.forename: Antonio
authors.initials: A
authors.lastname: Scilimati
authors.forename: Michela
authors.initials: M
authors.lastname: De Bellis
authors.forename: Annamaria
authors.initials: A
authors.lastname: De Luca
authors.forename: Diana Conte
authors.initials: DC
authors.lastname: Camerino
authors.forename: Maria Stefania
authors.initials: MS
authors.lastname: Sinicropi
authors.forename: Vincenzo
authors.initials: V
authors.lastname: Tortorella
mesh_terms: D015394:Molecular Structure; D018482:Muscle, Skeletal / Q000187:drug effects* / Q000378:metabolism; D009222:Myotonia; D026941:Sodium Channel Blockers / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D016677:Tocainide / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D026941:Sodium Channel Blockers; D016677:Tocainide