Synthesis of N1-(2,3,4-trimethoxybenzyl)-N2-{2-[(2,3,4-trimethoxybenzyl)amino]ethyl}-1,2-ethanediamine Organic Salts and their Cardiotropic Activity.

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Title: Synthesis of N1-(2,3,4-trimethoxybenzyl)-N2-{2-[(2,3,4-trimethoxybenzyl)amino]ethyl}-1,2-ethanediamine Organic Salts and their Cardiotropic Activity.
Authors: Mokrov, G. V.1 (AUTHOR) g.mokrov@gmail.com, Bobrovskii, S. I.1 (AUTHOR), Barchukov, V. V.1 (AUTHOR), Kryzhanovskii, S. A.1 (AUTHOR), Tsorin, I. B.1 (AUTHOR), Vititnova, M. B.1 (AUTHOR), Rebeko, A. G.1 (AUTHOR), Gudasheva, T. A.1 (AUTHOR)
Source: Pharmaceutical Chemistry Journal. Nov2022, Vol. 56 Issue 8, p1049-1053. 5p.
Subject Terms: *SALTS, *TETRAHYDROISOQUINOLINES, *CITRATES
Abstract: Organic salts of N1-(2,3,4-trimethoxybenzyl)-N2-{2-[(2,3,4-trimethoxybenzyl)amino]ethyl}-1,2-ethanediamine (I) (succinate ALM-802S and citrate ALM-802C) were obtained. These organic salts were found to retain completely the anti-arrhythmic and anti-ischemic properties of I trihydrochloride (ALM-802) in equimolar doses (2.15 – 2.75 mg/kg, i.v. administration). The new compounds belonged to toxicity class VI (low-toxicity substances). The LD50 values of the organic salts of I recalculated as the base corresponded to that of I trihydrochloride. The pH values of the organic salts of I were significantly higher than that of I trihydrochloride (5.5 – 5.8 vs. 3.5), which eliminated the local irritating action and undesirable organoleptic properties. [ABSTRACT FROM AUTHOR]
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ISSN:0091150X
DOI:10.1007/s11094-022-02751-7
Published in:Pharmaceutical Chemistry Journal
Language:English