ИСТИНА

Thiuronium salts have a number of valuable pharmaceutical properties, including the ability to inhibit the activity of the NMDA subtype of glutamate receptors and simultaneously activate the AMPA subtype of glutamate receptors, exhibit affinity for some alkali and alkaline earth metals, the ability to inhibit NO synthase, H2 and H3 histamine receptor agonists. In this work, we have proposed a new approach to the synthesis of thiuronium salts of ethylenediamine derivatives using aromatic aldehydes and an ammonia source. With the help of molecular modeling by the method of molecular dynamics, the possibility of binding to NMDA receptors was studied. The ability to bind calcium ions was also determined. A series of over 15 compounds have been tested for inhibition of glutamate-stimulated uptake, with at least 6 compounds shown to have this ability over the micromolar concentration range. The cytotoxicity of derivatives of thiuronium salts has been studied. It is shown that on four cell lines cytotoxicity is in the micromolar range. The structure of the conformation formed as a result of the polymerization of a crude preparation of tubulin and MAB aggregates was studied using an electron microscopic study.