In the continuing search for novel, biologically effective heterocyclic agents, several methods for the synthesis of 2‐heteroaryl‐[1,2,4]triazolo[1,5‐c]quinazoline‐5(6 H)‐thiones have been developed: thiolation of oxo derivatives, [5+1] cyclocondensation of [2‐(3‐heteroaryl‐[1,2,4]triazol‐5‐yl)phenyl]amines with carbon disulfide, potassium ethyl xanthogenate, or aryl isothiocyanates, and in situ reaction of 2‐isothiocyanatobenzonitrile with hydrazides. A series of N‐R‐2‐[(2‐heteroaryl‐[1,2,4]triazole‐[1,5‐c]quinazoline‐5‐yl)thio]acetamides were obtained by aminolysis of the corresponding acetic acids and alkylation of potassium thiolates with N‐R‐2‐chloroacetamides. It was established that some potassium thiolates, 4 a–4 d, 4 h, and 4 i, had high antibacterial activity against Staphylococcus aureus with a minimum inhibitory concentration of 12.5 μg mL−1 and minimum bactericidal concentration of 25 μg mL−1, which exceeded the values for trimethoprim. In addition, {2‐[3‐(1 H‐indole‐2‐yl)‐1 H‐1,2,4‐triazol‐5‐yl]phenyl}amine 2 i was investigated in the concentration range 100–0.01 μM at 59 lines of nine cancer cell types, and showed a mean effective concentration at 3.12–7.03 μM and cytotoxic effect at 15.56–67.38 μM. The possible mechanisms of activity were predicted by molecular docking studies to S. aureus dihydrofolate reductase and epidermal growth factor receptor kinase.

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Recent publication describes hydrolytic cleavage of azole and azine condensed cycles under the action of nucleophiles [1,3,6, 4,9,11,12,15,17,20,25,26,28,29]. It is known that kinetics of the reactions mentioned depends on basic properties of nucleophilic reagents. Strong nucleophiles (hydroxides and alkoxides of alkaline metals, hydrazine hydrate) easily react with the given substrates in the water or alcohol-water medium for 1 h and form products with high yields [4,15,20,25,26,28,29]. Moreover, water may play the role of a nucleophile in hydrolytic cleavage reactions. In this case the reaction proceeds for 1 h and needs acidic catalysis [1,6]. It has been noted that cleavage of the pyridine cycle of 2-aryl-[1,2,4]triazolo[1,5-c]quinazoline is insufficiently known in spite of potentially bioactive products of this transformation. In addition, products of the reactions mentioned may take a worth place in the process of development of approaches for forming new heterocyclic systems and drug discovery [2,8,13,18,19, 23,24].Moreover, we found reports where the hypoglycemic activity of derivatives of 1,2,4-triazole were described. Thus, A.K.Mohammed Iqbal and co-authors discussed in their research the hypoglycemic and hypolipidemic action of novel compounds, which molecules contained the thiazolidone fragment attached to the triazole cycle via phenoxyethenthiol "linker" groups [14]. 4-Methyl-3-(R-phenyl-,1-methyl-1Н-indol-4(5)-yl)-5-(R-phenyl-)-4H-1,2,4-triazoles as selective inhibitors of 11β-hydroxysteroid dehydrogenase 1 were described as prospective glucose-lowering agents by Susan D. Aster and co-authors [7], and "ELI LILLY and COMPANY" applied for patent series of 2-R 1 -4-R 2 -5-alkaryl-(alkheteryl-, aryl-(heteryl-) oxy-, aryl-(heteryl-)thio-, aryl-(heteryl-)amino-)-2,4-dihydro-3H-1,2,4-triazol-3-ones(thiones) with high affinity to nuclear hormonal receptors. They may be used for treating diabetes, cardiovascular disorders, obesity, Xsyndrome and gastrointestinal disorders [21, 22], etc.Thus, the aims of the present research were to study the peculiarities of the given type of the reaction, elucidation of the effect of o-, m-, p-substituted aryl moiety in position 2 of [1,2,4]triazolo [1,5-c]quinazolines on the process of the pyrimidine cycle hydrolytic cleavage, as well as the hypoglycemic action of the compounds synthesized.experimental part 1. Chemistry 1.1. General method. Melting points were determined in open capillary tubes and were uncorrected. The ele-

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The purpose of the study was to analyze the occupational morbidity in the Dnieper Economic Region, its structure in dynamics for 2015-2019, identify the main causes that lead to the formation of occupational pathology, and suggest ways to solve the problem. Material and methods. Based on the processing of the medical documentation of the clinic, the Ukrainian Research Institute of Industrial Medicine, we conducted a comparative analysis of occupational morbidity indicators in the dynamics of 2015-2019 was carried out taking into account the main forms of pathology and regional distribution. Results and discussion. The level of occupational morbidity among workers of the Dnieper Economic Region in 2015-2019 varies from 354 to 10307 cases. The leadership in the formation of professional pathology remains with the Dnipropetrovsk region, where large enterprises of the leading branches of heavy industry are located, in dangerous and harmful conditions of which a significant number of people work. In the structure of occupational morbidity, the first place is occupied by chronic obstructive pulmonary diseases of occupational etiology (31.7%), the second is cochlear neuritis (27.3%), the third is radiculopathy (23.7%), and the fourth is vibration disease (7.6%). Indicators of occupational morbidity indicate only the detection of occupational pathology. The statistics do not reflect the true situation, which is due to the imperfection of labor protection legislation, the lack of legal and economic sanctions for concealing occupational diseases, and the shortcomings of medical diagnostic and preventive work among workers. The solution to this problem, in our opinion, may consist in enhancing coordination of the entire complex of scientific and practical activities for the development and substantiation of strategies, tactics and implementation of national policies from the most important areas of occupational medicine. Conclusion. It is necessary to formulate a systematic approach to the prevention of occupational morbidity of the population, taking into account the characteristics of the current situation in the region and in the country as a whole. Comprehensive solution of problems in the health of workers, taking into account the interagency coordination of the system of measures, in the future will ensure the preservation of labor potential, prolong working life, and reduce general and occupational diseases