ПОХІДНІ 4-ГІДРАЗИНОХІНОЛІНУ ТА ЇХ БІОЛОГІЧНА АКТИВНІСТЬ (ОГЛЯД ЛІТЕРАТУРИ)

Abstract

The analysis of the literature about the biological activity of 4-hydrazinoquinolines derivatives was carried out. The variety of actions of this class of organic compounds was depicted. The most promising compounds are the ones that are associated with antimycobacterial and antimalarial activity. It is found out that the presence of substituents in the 6-th and / or 8-th position of the quinoline system increases, and in position 5 and 7 – reduces antimalarial and antibacterial activity. Studies have shown that 4-hydrazinequinolines have a fairly high toxicity, and the maintenance of electron-donating substituents leads to an increase in toxicity by 3-7 times. Their toxicity also increases in the series H <K <Na, which is associated with an increase in solubility in the above-mentioned compounds. 4-hydrazinoquinolines have a pronounced antioxidant effect, by blocking the hydrazino group on the α-ketoglutaric acid residue, the antioxidant effect is reduced, which is also due to their poor solubility in the media. Quinolinohydrazones have been investigated as transcriptase inhibitors, a retrovirus conversion enzyme. The inhibitory activity of the obtained compounds decreases in the series M-MulV> RAV-2> HIV-1. The cytotoxicity of these compounds was evaluated by means of Mosman’s analysis on a J774 cell line infected with BGC (bacille Calmette-Guerin). During this analysis, at R1 = 4-OMe, it was found to be non-cytotoxic to host cells at effective concentrations (MIK 2.5 mg / ml) to inhibit M. Tuberculosis growth. The effect of disodium salt of 2-methylquinolin-4-yl-hydrazone α-ketoglutaric acid on the synthesis of pigment in pigment-producing bacteria of the genera Pseudomonos and Serratia was studied. The maximum effect was observed at a concentration of 100 mg / L. Pigment-stimulating ability is enhanced in proportion to the concentration of 2-methyl-4-yl-hydrazone α-ketoglutaric acid in the culture medium (this trend is shown for cultures of Ps. Fluorescens iodinum, Pseudomonos fluorescens, S. Marcescens). The studied substances can be considered as the basis for the creation of new biologically active compounds.