Synthesis and Evaluation of Voltage-Gated Sodium Channel Blocking Pyrroline Derivatives Endowed with Both Antiarrhythmic and Antioxidant Activities.
Animals
Anti-Arrhythmia Agents
/ chemical synthesis
Antioxidants
/ chemical synthesis
Density Functional Theory
Fluoresceins
/ metabolism
Guinea Pigs
Humans
Molecular Structure
Pyrroles
/ chemical synthesis
Reperfusion Injury
/ drug therapy
Tumor Cells, Cultured
Voltage-Gated Sodium Channel Blockers
/ chemical synthesis
Voltage-Gated Sodium Channels
/ metabolism
Journal
ChemMedChem
ISSN: 1860-7187
Titre abrégé: ChemMedChem
Pays: Germany
ID NLM: 101259013
Informations de publication
Date de publication:
04 02 2021
04 02 2021
Historique:
received:
04
09
2020
pubmed:
6
10
2020
medline:
11
11
2021
entrez:
5
10
2020
Statut:
ppublish
Résumé
Under the hypothesis that cardioprotective agents might benefit from synergism between antiarrhythmic activity and antioxidant properties, a small series of mexiletine analogues were coupled with the 2,2,5,5-tetramethylpyrroline moiety, known for its antioxidant effect, in order to obtain dual-acting drugs potentially useful in the protection of the heart against post-ischemic reperfusion injury. The pyrroline derivatives reported herein were found to be more potent as antiarrhythmic agents than mexiletine and displayed antioxidant activity. The most interesting tetramethylpyrroline congener, a tert-butyl-substituted analogue, was at least 100 times more active as an antiarrhythmic than mexiletine.
Identifiants
pubmed: 33015979
doi: 10.1002/cmdc.202000692
doi:
Substances chimiques
Anti-Arrhythmia Agents
0
Antioxidants
0
Fluoresceins
0
Pyrroles
0
Voltage-Gated Sodium Channel Blockers
0
Voltage-Gated Sodium Channels
0
2',7'-dichlorodihydrofluorescein
106070-31-9
pyrroline
28350-87-0
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
578-588Subventions
Organisme : University of Bari Aldo Moro
Informations de copyright
© 2020 Wiley-VCH GmbH.
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