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Experimental, Theoretical and Biological Activity of a Triazonine- Derivative on Left Ventricular Pressure

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Background: There are data indicating that several azonine-derivatives may exert effects on some biological systems; however, there is very low information on the biological activity induced by these compounds on left ventricular pressure.

Objective: The aim of this study was to synthesize and evaluate the biological activity of new triazoninederivative on left ventricular pressure.

Material and Methods: The first stage involved: 1) preparation of two azepine-benzamide derivatives (Z or E) by reaction of the nitrobenzoyl azide with adrenosterone; and 2) reaction of (Z)-azepine-benzamide derivative with ethylenediamine to form the triazonine derivative. The structure of compounds was confirmed by spectroscopy and spectrometry data. The second stage involved the biologic activity on left ventricular pressure was evaluated in a model of rat heart isolated. In addition, some physicochemical parameters were evaluated to characterize the possible molecules involved in its effect.

Results: The results showed that only the triazonine increased left ventricular pressure via androgen receptor.

Conclusions: In conclusion, this phenomenon is conditioned by the functional groups involved in the chemical structure of triazonine derivative and their interaction with residues of amino acids involved on the androgen receptor surface.
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Keywords: Adrenosterone; androgen receptor; benzamide; ethylenediamine; triazonine derivative; ventricular pressure

Document Type: Research Article

Publication date: August 1, 2016

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  • Cardiovascular & Hematological Agents in Medicinal Chemistry aims to cover all the latest and outstanding developments in medicinal chemistry and rational drug design for the discovery of new Cardiovascular & Hematological Agents. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of current topics in Cardiovascular & Hematological medicinal chemistry.

    Cardiovascular & Hematological Agents in Medicinal Chemistry
    is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments in cardiovascular & hematological drug discovery.
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