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Objectives. Biogenic polyamines are widely present in nature. They are characteristic of both protozoan cells and multicellular organisms. These compounds have a wide range of biological functions and are necessary for normal growth and development of cells. Violation of polyamine homeostasis can cause significant abnormalities in cell functioning, provoking various pathological processes, including oncological and neuropsychiatric diseases. The impact on the “polyamine pathway” is an attractive basis for the creation of many pharmacological agents with a diverse spectrum of action. The purpose of this review is to summarize the results of the studies devoted to understanding the biological activity of compounds of the polyamine series, comparing their biological action with action on certain molecular targets. Due to the structural diversity of this group of substances, it is impossible to fully reflect the currently available data in one review. Therefore, in this work, the main attention is paid to the derivatives, acyclic saturated polyamines.Results. The following aspects are considered: biological functionality, biosynthesis and catabolism, cell transport, and localization of biogenic polyamines in the living systems. Structural analogs and derivatives of biogenic polyamines with antitumor, neuroprotective, antiarrhythmic, antiparasitic, antibacterial, and other biological activities are represented; the relationship between biological activity and the target of exposure is reflected. It was found that the nature of the substituent, the number of cationic centers, and the length of the polyamine chain have a great influence on the nature of the effect.Conclusions. At present, the use of polyamine structures is restrained by cytotoxicity and nonspecific toxic effects on the central nervous system. Further research in the field of biochemistry, cell transport, and a deeper understanding of receptor interaction mechanisms will help making polyamines as the basis for potential drug formulation.

A method for the synthesis of 2-(2-(dialkylamino)ethylamino)ethanols based on the epoxide ring opening in styrene oxide by N,N-disubstituted ethylenediamines was developed. It is shown that the opening of the oxirane ring by diamines in 2-propanol at room temperature occurs mainly according to the Krasusky rule at the bond between the oxygen atom and the less substituted carbon atom. A mixture of two products with the predominance of the secondary diamino alcohol up to 82% was obtained. It was found that the separation of the products by distillation or recrystallization does not allow obtaining pure isomers. The mixture of isomers was converted into dihydrochlorides by dry HCl in dioxane and diethyl ether. Pure 2-(2-(dialkylamino)ethylamino)-1-phenylethanols and 2-(2-(dialkylamino)ethylamino)-2-phenylethanols were separated by the first fractional recrystallization of a mixture of diaminoalcohol dihydrochlorides from a mixed solvent followed by alkalization of the products with an aqueous sodium hydroxide solution. The diamino alcohols were characterized by FT-IR, 1H- and 13C-NMR and HRMS-ESI.

The synthesis of a series of N-substituted arylheteraaliphatic amino amides was carried out to determine their antiarrhythmic activity. Styrene oxide was the initial compound for the synthesis. Its oxirane ring was opened with N,N-dialkylaminoethanols in the presence of alcoholates. It was found that the opening of the oxirane ring was carried out mainly according to the Krasusky rule on the bond between the oxygen atom and the less substituted carbon atom. A mixture of two products with the predominance of the secondary amino alcohol was created. The main product was separated by multiple vacuum distillations. 2-[2-(Dialkylamino) ethoxy]-1-phenylethanols were obtained and used in the Ritter reaction for the alkylation of benzonitrile in the presence of sulfuric acid to give N-{2-[2-(dialkylamino)ethoxy]-1-phenylethyl} benzamides. Biological tests of the obtained compounds were carried on the aconitine arrhythmia model out in rats. Procainamide, Quinidine, Lidocaine and Ethacyzin were used as the drugs. The findings in this study indicate that most of the obtained compounds have a low toxicity and expressed antiarrhythmic activity.

This article is devoted method of synthesis and study of the properties of (±)-trans-2- dialkylaminoethylaminocyclohexahols. It was found that the studied compounds are not toxic and have expressed antiarrhythmic properties. It was found that the explored compounds are low-toxicity substances having pronounced antiarrhythmic properties.

A series of trans-2-(substituted amino)-cyclohehyl esters have been synthesized and examined for pharmacological activity. Significant responses have been noted with these compounds as ant arrhythmic substances.

The preparative synthesis of bioactive arylheteroaliphatic N-substitued aminoamides based on the opening of epoxide ring of styrene oxide followed by acylation of diaminoalcohols with acyl chlorides, was developed.

The results of styrene oxide epoxide cycle cleavage by diamines were summarized. The effect of solvent on regioselectivity in the reaction of N,N-diethylene diamine was studied. It was established that the ratio of products correlates well with polarity parameters ЕТ and АN of pure solvents.