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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Main Authors:	Xue-Kun Liu, Long-Xu Ma, Zhi-Yu Wei, Xun Cui, Shi Zhan, Xiu-Mei Yin, Hu-Ri Piao
Format:	Article
Language:	English
Published:	MDPI AG 2017-02-01
Series:	Molecules
Subjects:	[1,2,4]triazolo[4,3-a] quinoxaline positive inotropic activity stroke volume atrium milrinone
Online Access:	http://www.mdpi.com/1420-3049/22/2/273

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spelling	doaj-9e37d57ab5c44608af991671c725fac52020-11-24T23:41:34ZengMDPI AGMolecules1420-30492017-02-0122227310.3390/molecules22020273molecules22020273Synthesis and Positive Inotropic Activity of [1,2,4]Triazolo[4,3-a] Quinoxaline Derivatives Bearing Substituted Benzylpiperazine and Benzoylpiperazine MoietiesXue-Kun Liu0Long-Xu Ma1Zhi-Yu Wei2Xun Cui3Shi Zhan4Xiu-Mei Yin5Hu-Ri Piao6Tonghua Normal University , College of Pharmaceutical and Food Science, Tonghua 134002, ChinaKey Laboratory of Natural Resources of Changbai Mountain & Functional Molecules, Ministry of Education, College of Pharmacy, Yanbian University, Yanji 133000, ChinaKey Laboratory of Natural Resources of Changbai Mountain & Functional Molecules, Ministry of Education, College of Pharmacy, Yanbian University, Yanji 133000, ChinaCollege of Medicine, Yanbian University, Yanji 133000, ChinaState Key Laboratory of Inorganic Synthesis and Preparative Chemistry, College of Chemistry, Jilin University, Changchun 130000, ChinaKey Laboratory of Natural Resources of Changbai Mountain & Functional Molecules, Ministry of Education, College of Pharmacy, Yanbian University, Yanji 133000, ChinaKey Laboratory of Natural Resources of Changbai Mountain & Functional Molecules, Ministry of Education, College of Pharmacy, Yanbian University, Yanji 133000, ChinaIn 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.http://www.mdpi.com/1420-3049/22/2/273[1,2,4]triazolo[4,3-a] quinoxalinepositive inotropic activitystroke volumeatriummilrinone
collection	DOAJ
language	English
format	Article
sources	DOAJ
author	Xue-Kun Liu Long-Xu Ma Zhi-Yu Wei Xun Cui Shi Zhan Xiu-Mei Yin Hu-Ri Piao
spellingShingle	Xue-Kun Liu Long-Xu Ma Zhi-Yu Wei Xun Cui Shi Zhan Xiu-Mei Yin Hu-Ri Piao Synthesis and Positive Inotropic Activity of [1,2,4]Triazolo[4,3-a] Quinoxaline Derivatives Bearing Substituted Benzylpiperazine and Benzoylpiperazine Moieties Molecules [1,2,4]triazolo[4,3-a] quinoxaline positive inotropic activity stroke volume atrium milrinone
author_facet	Xue-Kun Liu Long-Xu Ma Zhi-Yu Wei Xun Cui Shi Zhan Xiu-Mei Yin Hu-Ri Piao
author_sort	Xue-Kun Liu
title	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_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_sort	synthesis and positive inotropic activity of [1,2,4]triazolo[4,3-a] quinoxaline derivatives bearing substituted benzylpiperazine and benzoylpiperazine moieties
publisher	MDPI AG
series	Molecules
issn	1420-3049
publishDate	2017-02-01
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.
topic	[1,2,4]triazolo[4,3-a] quinoxaline positive inotropic activity stroke volume atrium milrinone
url	http://www.mdpi.com/1420-3049/22/2/273
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Synthesis and Positive Inotropic Activity of [1,2,4]Triazolo[4,3-a] Quinoxaline Derivatives Bearing Substituted Benzylpiperazine and Benzoylpiperazine Moieties

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