Synthesis and Positive Inotropic Activity of [1,2,4]Triazolo[4,3-a] Quinoxaline Derivatives Bearing Substituted Benzylpiperazine and Benzoylpiperazine Moieties

In an attempt to search for more potent positive inotropic agents, two series of [1,2,4]triazolo[4,3-a] quinoxaline derivatives bearing substituted benzylpiperazine and benzoylpiperazine moieties were synthesized and their positive inotropic activities evaluated by measuring left atrial stroke volum...

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Autores principales: Liu, Xue-Kun, Ma, Long-Xu, Wei, Zhi-Yu, Cui, Xun, Zhan, Shi, Yin, Xiu-Mei, Piao, Hu-Ri
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2017
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6155749/
https://www.ncbi.nlm.nih.gov/pubmed/28208674
http://dx.doi.org/10.3390/molecules22020273
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author Liu, Xue-Kun
Ma, Long-Xu
Wei, Zhi-Yu
Cui, Xun
Zhan, Shi
Yin, Xiu-Mei
Piao, Hu-Ri
author_facet Liu, Xue-Kun
Ma, Long-Xu
Wei, Zhi-Yu
Cui, Xun
Zhan, Shi
Yin, Xiu-Mei
Piao, Hu-Ri
author_sort Liu, Xue-Kun
collection PubMed
description In an attempt to search for more potent positive inotropic agents, two series of [1,2,4]triazolo[4,3-a] quinoxaline derivatives bearing substituted benzylpiperazine and benzoylpiperazine moieties were synthesized and their positive inotropic activities evaluated by measuring left atrial stroke volume in isolated rabbit heart preparations. Several compounds showed favorable activities compared with the standard drug, milrinone. Compound 6c was the most potent agent, with an increased stroke volume of 12.53% ± 0.30% (milrinone: 2.46% ± 0.07%) at 3 × 10(−5) M. The chronotropic effects of compounds having considerable inotropic effects were also evaluated.
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spelling pubmed-61557492018-11-13 Synthesis and Positive Inotropic Activity of [1,2,4]Triazolo[4,3-a] Quinoxaline Derivatives Bearing Substituted Benzylpiperazine and Benzoylpiperazine Moieties Liu, Xue-Kun Ma, Long-Xu Wei, Zhi-Yu Cui, Xun Zhan, Shi Yin, Xiu-Mei Piao, Hu-Ri Molecules Article In an attempt to search for more potent positive inotropic agents, two series of [1,2,4]triazolo[4,3-a] quinoxaline derivatives bearing substituted benzylpiperazine and benzoylpiperazine moieties were synthesized and their positive inotropic activities evaluated by measuring left atrial stroke volume in isolated rabbit heart preparations. Several compounds showed favorable activities compared with the standard drug, milrinone. Compound 6c was the most potent agent, with an increased stroke volume of 12.53% ± 0.30% (milrinone: 2.46% ± 0.07%) at 3 × 10(−5) M. The chronotropic effects of compounds having considerable inotropic effects were also evaluated. MDPI 2017-02-11 /pmc/articles/PMC6155749/ /pubmed/28208674 http://dx.doi.org/10.3390/molecules22020273 Text en © 2017 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Liu, Xue-Kun
Ma, Long-Xu
Wei, Zhi-Yu
Cui, Xun
Zhan, Shi
Yin, Xiu-Mei
Piao, Hu-Ri
Synthesis and Positive Inotropic Activity of [1,2,4]Triazolo[4,3-a] Quinoxaline Derivatives Bearing Substituted Benzylpiperazine and Benzoylpiperazine Moieties
title Synthesis and Positive Inotropic Activity of [1,2,4]Triazolo[4,3-a] Quinoxaline Derivatives Bearing Substituted Benzylpiperazine and Benzoylpiperazine Moieties
title_full Synthesis and Positive Inotropic Activity of [1,2,4]Triazolo[4,3-a] Quinoxaline Derivatives Bearing Substituted Benzylpiperazine and Benzoylpiperazine Moieties
title_fullStr Synthesis and Positive Inotropic Activity of [1,2,4]Triazolo[4,3-a] Quinoxaline Derivatives Bearing Substituted Benzylpiperazine and Benzoylpiperazine Moieties
title_full_unstemmed Synthesis and Positive Inotropic Activity of [1,2,4]Triazolo[4,3-a] Quinoxaline Derivatives Bearing Substituted Benzylpiperazine and Benzoylpiperazine Moieties
title_short Synthesis and Positive Inotropic Activity of [1,2,4]Triazolo[4,3-a] Quinoxaline Derivatives Bearing Substituted Benzylpiperazine and Benzoylpiperazine Moieties
title_sort synthesis and positive inotropic activity of [1,2,4]triazolo[4,3-a] quinoxaline derivatives bearing substituted benzylpiperazine and benzoylpiperazine moieties
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6155749/
https://www.ncbi.nlm.nih.gov/pubmed/28208674
http://dx.doi.org/10.3390/molecules22020273
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