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Antiarrhythmic and antioxidant activity of novel pyrrolidin-2-one derivatives with adrenolytic properties

A series of novel pyrrolidin-2-one derivatives (17 compounds) with adrenolytic properties was evaluated for antiarrhythmic, electrocardiographic and antioxidant activity. Some of them displayed antiarrhythmic activity in barium chloride-induced arrhythmia and in the rat coronary artery ligation-repe...

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Autores principales: Sapa, Jacek, Nowaczyk, Alicja, Kulig, Katarzyna
Formato: Texto
Lenguaje:English
Publicado: Springer-Verlag 2010
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3016165/
https://www.ncbi.nlm.nih.gov/pubmed/20949258
http://dx.doi.org/10.1007/s00210-010-0566-x
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author Sapa, Jacek
Nowaczyk, Alicja
Kulig, Katarzyna
author_facet Sapa, Jacek
Nowaczyk, Alicja
Kulig, Katarzyna
author_sort Sapa, Jacek
collection PubMed
description A series of novel pyrrolidin-2-one derivatives (17 compounds) with adrenolytic properties was evaluated for antiarrhythmic, electrocardiographic and antioxidant activity. Some of them displayed antiarrhythmic activity in barium chloride-induced arrhythmia and in the rat coronary artery ligation-reperfusion model, and slightly decreased the heart rate, prolonged P–Q, Q–T intervals and QRS complex. Among them, compound EP-40 (1-[2-hydroxy-3-[4-[(2-hydroxyphenyl)piperazin-1-yl]propyl]pyrrolidin-2-one showed excellent antiarrhythmic activity. This compound had significantly antioxidant effect, too. The present results suggest that the antiarrhythmic effect of compound EP-40 is related to their adrenolytic and antioxidant properties. A biological activity prediction using the PASS software shows that compound EP-35 and EP-40 can be characterized by antiischemic activity; whereas, compound EP-68, EP-70, EP-71 could be good tachycardia agents.
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spelling pubmed-30161652011-02-04 Antiarrhythmic and antioxidant activity of novel pyrrolidin-2-one derivatives with adrenolytic properties Sapa, Jacek Nowaczyk, Alicja Kulig, Katarzyna Naunyn Schmiedebergs Arch Pharmacol Original Article A series of novel pyrrolidin-2-one derivatives (17 compounds) with adrenolytic properties was evaluated for antiarrhythmic, electrocardiographic and antioxidant activity. Some of them displayed antiarrhythmic activity in barium chloride-induced arrhythmia and in the rat coronary artery ligation-reperfusion model, and slightly decreased the heart rate, prolonged P–Q, Q–T intervals and QRS complex. Among them, compound EP-40 (1-[2-hydroxy-3-[4-[(2-hydroxyphenyl)piperazin-1-yl]propyl]pyrrolidin-2-one showed excellent antiarrhythmic activity. This compound had significantly antioxidant effect, too. The present results suggest that the antiarrhythmic effect of compound EP-40 is related to their adrenolytic and antioxidant properties. A biological activity prediction using the PASS software shows that compound EP-35 and EP-40 can be characterized by antiischemic activity; whereas, compound EP-68, EP-70, EP-71 could be good tachycardia agents. Springer-Verlag 2010-10-15 2011 /pmc/articles/PMC3016165/ /pubmed/20949258 http://dx.doi.org/10.1007/s00210-010-0566-x Text en © The Author(s) 2010 https://creativecommons.org/licenses/by-nc/4.0/ This article is distributed under the terms of the Creative Commons Attribution Noncommercial License which permits any noncommercial use, distribution, and reproduction in any medium, provided the original author(s) and source are credited.
spellingShingle Original Article
Sapa, Jacek
Nowaczyk, Alicja
Kulig, Katarzyna
Antiarrhythmic and antioxidant activity of novel pyrrolidin-2-one derivatives with adrenolytic properties
title Antiarrhythmic and antioxidant activity of novel pyrrolidin-2-one derivatives with adrenolytic properties
title_full Antiarrhythmic and antioxidant activity of novel pyrrolidin-2-one derivatives with adrenolytic properties
title_fullStr Antiarrhythmic and antioxidant activity of novel pyrrolidin-2-one derivatives with adrenolytic properties
title_full_unstemmed Antiarrhythmic and antioxidant activity of novel pyrrolidin-2-one derivatives with adrenolytic properties
title_short Antiarrhythmic and antioxidant activity of novel pyrrolidin-2-one derivatives with adrenolytic properties
title_sort antiarrhythmic and antioxidant activity of novel pyrrolidin-2-one derivatives with adrenolytic properties
topic Original Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3016165/
https://www.ncbi.nlm.nih.gov/pubmed/20949258
http://dx.doi.org/10.1007/s00210-010-0566-x
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