Pruhlo Y. Synthesis and biological properties of 3-S-substituted 5-Alk- (Ar-, Het-)-4(H)-R-1,2,4-triazole

The dissertation is devoted to the search of biologically active compounds among 3-S-substituted 5-Alk-(Ar-, Het-)-4(H)-R-1,2,4-triazole. The basis of this work was the search for substances with enhanced pharmacological activity and increased safety which could become the basis for the creation of a new original domestic medicinal product. When carrying out pharmacological screening of 231 compounds 1,2,4-triazole derivatives, a number of compounds with high antihypoxic, antioxidant, actoprotective, antidepressant, anxiolytic and diuretic activities were detected. The choice of «leader compound» has been substantiated, for which acute toxicity has been studied and a number of toxicometric parameters have been established. Methylammonium 2-(4-amino-5-phenyl-4H-1,2,4-triazole-3-ylsulfanyl)acetate («Methamitrile») was recommended for clinical trials as a promising diuretic drug. Acute, subchronic toxicity and specific activity have been studied for Methamitrile, pharmacokinetic parameters have been established, dosage has been substantiated, a dosage formulation has been developed, a draft design specification has been developed, and synthesis has been tested in the production conditions.