Influence of Bis-(2,3,4-Trimethoxyphenyl)Azaalkanes Central Atom Type on Their Cardiotropic Activity.

Autor: Mokrov, G. V., Vorobieva, T. Yu., Birukova, V. E., Barchukova, E. I., Tsorin, I. B., Vititnova, M. B., Rebeko, A. G., Kryzhanovskiy, S. A., Gudasheva, T. A.
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Zdroj: Pharmaceutical Chemistry Journal; Dec2023, Vol. 57 Issue 9, p1350-1355, 6p
Abstrakt: New compounds of bis(2,3,4-trimethoxyphenyl)azaalkanes differing in the structure of the central atom were obtained. The anti-ischemic and antiarrhythmic activities of the new compounds were studied. Their absorption, distribution, metabolism, and excretion (ADME) characteristics were analyzed. Replacement of the central N atom by other atoms (O, C, S) had practically no effect on their antiarrhythmic and anti-ischemic properties but improved their calculated oral bioavailability. The promising compound ALM-863 {2,2′-oxybis[N-(2,3,4-trimethoxybenzyl)ethane-1-amine] dihydrochloride} at a dose of 3 mg/kg (i.v.) completely repeated the spectrum of cardiotropic properties of the ALM-802 prototype, was less toxic and surpassed it in terms of calculated pharmacokinetic parameters, and was selected. [ABSTRACT FROM AUTHOR]
Databáze: Complementary Index