Синтезированы новые конденсированные пиримидиновые соединения, имеющие бензаннелированную хиназолиновую структуру с различными функциональными заместителями в положении N3 пиримидиновой системы: 2-метил-3-(2-фенил-2-оксоэтил)хиназолин-4(3H)-он; 3-(2-трет-бутил-2-оксоэтил)хиназолин-4(3H)-он; 3-[2-(1-нафтил)-2-оксоэтил]-6-бромхиназолин-4(3H)-он; 3-(2-изопропилокси-2-оксоэтил)хиназолин-4(3H)-он; 3-[2-[(4,6-диметилпиримидин-2-ил)амино]-2-оксоэтил]хиназолин-4(3H)-он. Установлено, что новые производные хиназолина оказывают корригирующее влияние на процессы пролиферации в иммунокомпетентных органах, восстанавливая количество спленоцитов и тимоцитов на фоне циклофосфановой иммунодепрессии у мышей линии СВА обоего пола 3 – 4-месячного возраста.

— In this study we have investigated the effects of melanocortins (group analogs of neuropeptides) on the psychoemotional state of rats under conditions of experimental social stress. The study was carried out on male rats which were injected intraperitoneally for 20 days with the neuropeptide drugs Semax and ACTH(6-9)-ProGly-Pro at a dose of 100 μg/kg/day starting from the 1st day of stress exposure. The psychoemotional state of the animals was evaluated by means of the behavioral test of elevated cruciform maze. It was found that intraperitoneal administration of neuropeptides (Semax, ACTH(6-9)- Pro-Gly-Pro) helps to reduce high anxiety levels in animals both with aggressive and submissive types of behavior under conditions of experimental social stress via their psychomodulatory effects.

Quinazolin-4(3H)-one derivatives exhibiting a wide spectrum of a pharmacological activity, represent a promising class of substances used to obtain antibacterial agents, which is especially important in the context of the emergence of pathogenic microorganisms’ resistance to drugs used in medicine. It has been proved that compounds having a naphthyl radical in the molecule, as well as an amide group bound to the benzene ring as quinazolinone substituents, are characterized by a pronounced antimicrobial activity against Staphylococcus aureus and Streptococcus pneumoniae.The aim of the research is a primary microbiological screening of the in vitro antimicrobial activity of new quinazolin-4(3H)-one derivatives against Staphylococcus aureus and Streptococcus pneumoniae, as well as the assessment of the relationship between the pharmacological effect and the structural transformation of the substance molecule, lipophilicity and the possibility of forming resistance to them.Materials and methods. The experimental studies have been carried out using well-known nosocomial pathogens of infectious and inflammatory diseases Staphylococcus aureus and Streptococcus pneumoniae by a serial dilution method.Results. A compound containing a naphthyl radical in its structure, which contributes to an increase in the hydrophobicity of the substance and its solubility in the membrane of a bacterial cell, has a bacteriostatic effect against both Staphylococcus aureus and Streptococcus pneumoniae. A similar pharmacological effect is exhibited by a derivative with an amide group as a substituent of the quinazolinone nucleus linked to a phenyl radical, which probably contributes to an increase in the degree of binding to active sites of enzymes involved in the DNA replication, and protein synthesis. Obviously, the increased lipophilicity, which promotes better binding to the efflux protein, cannot serve as objective characteristics of the emergence possibility of the pathogen’s resistance to this substance.Conclusion. Among the synthesized compounds, the leading substances that exhibit an antimicrobial activity against Staphylococcus aureus and Streptococcus pneumonia, have been identified. The assessment of the chemical structure made it possible to substantiate their pharmacological action and draw conclusions about the possibility of developing resistance to it in microbial cells.

The experiment is devoted to the study of the effect of neuropeptides on the psychoemotional state of rats exposed to experimental social stress. In the process of modeling social stress, inter-male confrontations were observed, as a result of which groups of animals with aggressive and submissive types of behavior were formed.

Aim of the study was to screen the antimicrobial activity of pyrimidine derivative 3-[2-(1-naphthyl)-2-oxoethyl]-6-bromoquinazoline-4(3H)-oh with laboratory cipher VMA–13–06 in relation to pathogenic and opportunistic flora. Material and methods. Antimicrobial activity of VMA–13–06 was established in vitro against strains of Staphylococcus aureus, Klebsiella pneumonia, Streptococcus pyogenes, Escherichia coli, Acinetobacter baumannii and Citrobacter freundii by the method of serial dilutions, by forming rows with different concentrations of the compound under study. Results. VMA–13–06 was found to exhibit high antibacterial activity against S. aureus, S. pyogenes, E. coli and K. pneumonia at concentrations of 128 and 64 μg/ml comparable to the activity of the comparison drug norfloxacin. At a concentration of 32 μg/ml, the studied derivative is highly active against S. aureus and S. pyogenes and shows average activity against E. coli and K. pneumonia. The compound VMA–13–06 in dilution from 16 to 4 μg/ml is moderately active against the above-mentioned microorganisms. At concentrations from 2 to 0.25 μg/ml, the pyrimidine derivative is inactive against S. aureus, S. pyogenes, E. coli and K. pneumonia, in all dilutions – against C. freundii and A. baumannii. Conclusions. The results of a screening study indicate a pronounced bactericidal effect of VMA–13–06 against S. aureus, S. pyogenes, E. coli и K. pneumonia comparable to the comparison drug norfloxacin.