Title: Influence of Bis-(2,3,4-Trimethoxyphenyl)Azaalkanes Central Atom Type on Their Cardiotropic Activity.
Authors: 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.
Abstract: 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.
Subjects: PHARMACOKINETICS; BIOAVAILABILITY; EXCRETION; ATOMS; METABOLISM; ABSORPTION
Publication: Pharmaceutical Chemistry Journal, 2023, Vol 57, Issue 9, p1350
ISSN: 0091-150X
Publication type: Academic Journal
DOI: 10.1007/s11094-023-02996-w

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

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.