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Molecules 2017, 22(2), 273; doi:10.3390/molecules22020273

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

1
Tonghua Normal University , College of Pharmaceutical and Food Science, Tonghua 134002, China
2
Key Laboratory of Natural Resources of Changbai Mountain & Functional Molecules, Ministry of Education, College of Pharmacy, Yanbian University, Yanji 133000, China
3
College of Medicine, Yanbian University, Yanji 133000, China
4
State Key Laboratory of Inorganic Synthesis and Preparative Chemistry, College of Chemistry, Jilin University, Changchun 130000, China
These authors contributed equally to this work.
*
Authors to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 15 January 2017 / Revised: 7 February 2017 / Accepted: 8 February 2017 / Published: 11 February 2017
(This article belongs to the Section Medicinal Chemistry)
View Full-Text   |   Download PDF [1063 KB, uploaded 11 February 2017]   |  

Abstract

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. View Full-Text
Keywords: [1,2,4]triazolo[4,3-a] quinoxaline; positive inotropic activity; stroke volume; atrium; milrinone [1,2,4]triazolo[4,3-a] quinoxaline; positive inotropic activity; stroke volume; atrium; milrinone
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Liu, X.-K.; Ma, L.-X.; Wei, Z.-Y.; Cui, X.; Zhan, S.; Yin, X.-M.; Piao, H.-R. Synthesis and Positive Inotropic Activity of [1,2,4]Triazolo[4,3-a] Quinoxaline Derivatives Bearing Substituted Benzylpiperazine and Benzoylpiperazine Moieties. Molecules 2017, 22, 273.

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