Literature DB >> 18342401

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

Alessia Catalano1, Alessia Carocci, Filomena Corbo, Carlo Franchini, Marilena Muraglia, Antonio Scilimati, Michela De Bellis, Annamaria De Luca, Diana Conte Camerino, Maria Stefania Sinicropi, Vincenzo Tortorella.   

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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Year:  2008        PMID： 18342401     DOI： 10.1016/j.ejmech.2008.01.023

Source DB:  PubMed          Journal:  Eur J Med Chem        ISSN： 0223-5234            Impact factor:   6.514


  7 in total

1.  Myotonia congenita and myotonic dystrophy: surveillance and management.

Authors:  Allison Conravey; Lenay Santana-Gould
Journal:  Curr Treat Options Neurol       Date:  2010-01       Impact factor: 3.598

2.  Bioisosteric Modification of To042: Synthesis and Evaluation of Promising Use-Dependent Inhibitors of Voltage-Gated Sodium Channels.

Authors:  Gualtiero Milani; Maria Maddalena Cavalluzzi; Concetta Altamura; Antonella Santoro; Mariagrazia Perrone; Marilena Muraglia; Nicola Antonio Colabufo; Filomena Corbo; Elisabetta Casalino; Carlo Franchini; Isabella Pisano; Jean-François Desaphy; Antonio Carrieri; Alessia Carocci; Giovanni Lentini
Journal:  ChemMedChem       Date:  2021-10-05       Impact factor: 3.540

Review 3.  The non-dystrophic myotonias: molecular pathogenesis, diagnosis and treatment.

Authors:  E Matthews; D Fialho; S V Tan; S L Venance; S C Cannon; D Sternberg; B Fontaine; A A Amato; R J Barohn; R C Griggs; M G Hanna
Journal:  Brain       Date:  2009-11-16       Impact factor: 13.501

4.  Searching for novel anti-myotonic agents: pharmacophore requirement for use-dependent block of skeletal muscle sodium channels by N-benzylated cyclic derivatives of tocainide.

Authors:  Annamaria De Luca; Michela De Bellis; Filomena Corbo; Carlo Franchini; Marilena Muraglia; Alessia Catalano; Alessia Carocci; Diana Conte Camerino
Journal:  Neuromuscul Disord       Date:  2011-07-29       Impact factor: 4.296

5.  Increased sodium channel use-dependent inhibition by a new potent analogue of tocainide greatly enhances in vivo antimyotonic activity.

Authors:  Michela De Bellis; Roberta Carbonara; Julien Roussel; Alessandro Farinato; Ada Massari; Sabata Pierno; Marilena Muraglia; Filomena Corbo; Carlo Franchini; Maria Rosaria Carratù; Annamaria De Luca; Diana Conte Camerino; Jean-François Desaphy
Journal:  Neuropharmacology       Date:  2016-10-13       Impact factor: 5.250

6.  Dual Action of Mexiletine and Its Pyrroline Derivatives as Skeletal Muscle Sodium Channel Blockers and Anti-oxidant Compounds: Toward Novel Therapeutic Potential.

Authors:  Michela De Bellis; Francesca Sanarica; Alessia Carocci; Giovanni Lentini; Sabata Pierno; Jean-François Rolland; Diana Conte Camerino; Annamaria De Luca
Journal:  Front Pharmacol       Date:  2018-01-12       Impact factor: 5.810

7.  Three-dimensional structure of human cyclooxygenase (hCOX)-1.

Authors:  Morena Miciaccia; Benny Danilo Belviso; Mariaclara Iaselli; Gino Cingolani; Savina Ferorelli; Marianna Cappellari; Paola Loguercio Polosa; Maria Grazia Perrone; Rocco Caliandro; Antonio Scilimati
Journal:  Sci Rep       Date:  2021-02-22       Impact factor: 4.379
  7 in total

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