Study of ALM-802 orto-alkoxi analogues cardiotropic activity
https://doi.org/10.37489/2587-7836-2019-4-18-23
Abstract
New ortho-alkoxy analogs of the compound ALM-802 1a (N1-(2-methoxybenzyl)-N2-[2-((2-methoxybenzyl)amino)ethyl]ethane-1,2-diamine trihydrochloride) and 1b (N1-(2-ethoxybenzyl)-N2-[2-((2-ethoxybenzyl)amino)ethyl]ethane-1,2-diamine trihydrochloride), which differ from it by the presence of alkoxy groups in the phenyl rings only in the ortho positions. It was established that these structural changes lead to the disappearance of anti-ischemic activity. At the same time, antiarrhythmic activity was revealed in compound 1b on the models of aconitine and calcium chloride arrhythmias in rats (1 mg / kg, intravenously), which was absent in 1a.
About the Authors
G. V. MokrovRussian Federation
Mokrov Grigory, SPIN code: 8755-7666, Candidate of Chemical Sciences, Leading Researcher of the fine organic synthesis laboratory at the medicinal chemistry department, Moscow
A. M. Likhosherstov
Russian Federation
Likhosherstov Arkady, SPIN code: 1980-7331, Candidate of Chemical Sciences, Consultant of drug chemistry department, Moscow
V. V. Barchukov
Russian Federation
Barchukov Vladimir, SPIN code: 6743-4280, Research Scientist of laboratory of pharmacological screening, Moscow
V. N. Stolyaruk
Russian Federation
Stolyaruk Valeriy, SPIN code: 3405-8229, PhD, Senior Researcher Scientist of laboratory of pharmacological screening, Moscow
I. B. Tsorin
Russian Federation
Tsorin Iosif, SPIN code: 4015-3025, Doctor of Biological Sciences, Leading researcher of laboratory of pharmacological screening, Moscow
M. B. Vititnova
Russian Federation
Vititnova Marina, SPIN code: 1901-8919, Candidate of Biologicall Sciences, Senior researcher scientist of laboratory of pharmacological screening, Moscow
S. A. Kryzhanovskiy
Russian Federation
Kryzhanovskii Sergey, SPIN code: 6596-4865, Doctor of Medical Sciences, Head of laboratory of pharmacological screening, Moscow
T. A. Gudasheva
Russian Federation
Gudasheva Tatiana, SPIN code: 4970-0006, Doctor of Biological Sciences, professor, RAS corresponding member, Head of medicinal chemistry department, Moscow
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Review
For citations:
Mokrov G.V., Likhosherstov A.M., Barchukov V.V., Stolyaruk V.N., Tsorin I.B., Vititnova M.B., Kryzhanovskiy S.A., Gudasheva T.A. Study of ALM-802 orto-alkoxi analogues cardiotropic activity. Pharmacokinetics and Pharmacodynamics. 2019;(4):18-23. (In Russ.) https://doi.org/10.37489/2587-7836-2019-4-18-23