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Anti-Inflammatory & Anti-Allergy Agents in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1871-5230
ISSN (Online): 1875-614X

Research Article

Synthesis and Biological Activity of the Pyridine-hexacyclic-steroid Derivative on a Heart Failure Model

Author(s): Figueroa-Valverde Lauro*, López-Ramos Maria, Díaz-Cedillo Francisco, Rosas-Nexticapa Marcela*, Mateu-Armad Maria Virginia, Alvarez-Ramirez Magdalena, Lopez-Gutierrez Tomas and Arakachi-Cruz Idalia

Volume 21, Issue 1, 2022

Published on: 18 February, 2022

Page: [34 - 45] Pages: 12

DOI: 10.2174/1871523021666211222125403

Price: $65

Abstract

Background: Several drugs with inotropic activity have been synthesized; however, there is very little information on biological activity exerted by steroid derivatives in the cardiovascular system.

Objective: The aim of this research was to prepare a steroid-pyridine derivative to evaluate the effect it exerts on left ventricular pressure and characterize its molecular interaction.

Methods: The first stage was carried out through the synthesis of a steroid-pyridine derivative using some chemical strategies. The second stage involved the evaluation of the biological activity of the steroid-pyridine derivative on left ventricular pressure using a model of heart failure in the absence or presence of the drugs, such as flutamide, tamoxifen, prazosin, metoprolol, indomethacin, and nifedipine.

Results: The results showed that steroid-pyridine derivative increased left ventricular pressure in a dose-dependent manner (0.001-100 nM); however, this phenomenon was significantly inhibited only by nifedipine at a dose of 1 nM. These results indicate that positive inotropic activity produced by the steroid-pyridine derivative was via calcium channel activation. Furthermore, the biological activity exerted by the steroid-pyridine derivative on the left ventricle produces changes in cAMP concentration.

Conclusion: It is noteworthy that positive inotropic activity produced by this steroid-pyridine derivative involves a different molecular mechanism compared to other positive inotropic drugs. Therefore, this steroid could be a good candidate for the treatment of heart failure.

Keywords: Steroid, pyridine, biological, activity, ventricular, pressure.

Graphical Abstract

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