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A series of azolo[5,1-c][1,2,4]triazines containing a cyano group were prepared as analogs of the drug Triazavirin (riamilovir). Sodium 3-cyano-7-methylsulfanyl-4-oxo-4H-[1,2,4]triazolo[5,1-c][1,2,4]triazin-1-ide was tested for antiviral activity against the viruses of tick-borne encephalitis, Venezuelan equine encephalomyelitis, and the Eastern equine encephalomyelitis using porcine embryonic kidney cell model and mouse model according to the emergency prophylaxis model and therapy model. The general toxicity of this compound was also characterized.

The article presents the results of a study of the neurotoxicological profile of the new compound AB-19, acting on collagen glycation end products (AGE) and their receptors (RAGE), for the prevention and treatment of diabetes complications. The multi-test method «S. Irwin» was used. The test results were evaluated in parallel groups receiving the substance in doses starting with the average effective dose (ED50) and with a multiple increase by 5, 10, 20 and 50 times. It was found that the compound AB-19 in doses of 20, 100 and 200 mg / kg does not affect the functional and behavioral status of animals. However, with an increase to 400 mg / kg, typical manifestations of intoxication were observed: a decrease in muscle tone, hypothermia, sedation, tachypnea. As a result of the study, it was revealed that the neurotoxicological properties of the compound AB-19 are characterized by dose-dependent activity. A minimum toxic dose of 400 mg / kg ≤ Tdmin ≤ 1000 mg / kg was also indicated.

The nucleophilic susbstitution of nitro group in [1,2,4]triazolo[5,1-c][1,2,4]triazinones upon treatment with cysteine and glutathione was studied as a model for the interaction with thiol groups of virus proteins, which mimics the metabolic transformations of antiviral drug Triazavirin® and its derivatives.

Inhibition of the dipeptidyl peptidase-4 (DPP4) enzyme activity and prevention of advanced glycation end (AGE) products formation represents a reliable approach to achieve control over hyperglycemia and the associated pathogenesis of diabetic vascular complications. In the frames of this research study, several triazolo- and pyrazolotriazines were synthesized and evaluated as inhibitors of AGE products formation, DPP4, glycogen phosphorylase and α-glucosidase activities, as well as AGE cross-link breakers. From the two considered classes of heterocyclic compounds, the pyrazolotriazines showed the highest potency as antiglycating agents and DPP4 inhibitors. Structure-activity relationships (SAR) for these compounds, which can be considered as potential drugs for the treatment of type 2 diabetes, were evaluated.

Inhibition of the dipeptidyl peptidase-4 (DPP4) enzyme activity and prevention of advanced glycation end (AGE) products formation represents a reliable approach to achieve control over hyperglycemia and the associated pathogenesis of diabetic vascular complications. In the frames of this research study, several triazolo- and pyrazolotriazines were synthesized and evaluated as inhibitors of AGE products formation, DPP4, glycogen phosphorylase and α-glucosidase activities, as well as AGE cross-link breakers. From the two considered classes of heterocyclic compounds, the pyrazolotriazines showed the highest potency as antiglycating agents and DPP4 inhibitors. Structure-activity relationships (SAR) for these compounds, which can be considered as potential drugs for the treatment of type 2 diabetes, were evaluated.