TY - JOUR
T1 - Experimental, theoretical and biological activity of a triazonine-derivative on left ventricular pressure
AU - Figueroa-Valverde, Lauro
AU - López-Ramos, Maria
AU - Rosas-Nexticapa, Marcela
AU - Herrera-Meza, Socorro
AU - Díaz-Cedillo, Francisco
AU - García-Cervera, Elodia
AU - Pool-Gómez, Eduardo
AU - Garcia-Camacho, Tania
AU - Aguilar-Villarino, Angel
N1 - Publisher Copyright:
© 2016 Bentham Science Publishers.
PY - 2016
Y1 - 2016
N2 - 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 triazonine-derivative 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.
AB - 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 triazonine-derivative 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.
KW - Adrenosterone
KW - Androgen receptor
KW - Benzamide
KW - Ethylenediamine
KW - Triazonine derivative
KW - Ventricular pressure
UR - http://www.scopus.com/inward/record.url?scp=85027688278&partnerID=8YFLogxK
U2 - 10.2174/1871525715666161123115308
DO - 10.2174/1871525715666161123115308
M3 - Artículo
C2 - 27889993
SN - 1871-5257
VL - 14
SP - 125
EP - 133
JO - Cardiovascular and Hematological Agents in Medicinal Chemistry
JF - Cardiovascular and Hematological Agents in Medicinal Chemistry
IS - 2
ER -