Objects - synthesis, research of physical, chemical and pharmacological properties of new biologically active substances - derivatives of 2,4-dihydro-3H-1,2,4-triazol-3-thione; the goal is to select, based on the studies in silico, of the basic structures of 1,2,4-triazole-3-thione and to direct the synthesis of new potential biologically active substances (BAS) on the basis of them - 4,5-disubstituted anilides (1,2,4-triazole (4H) -3-yl) thioglycol acids, determination of their physico-chemical and pharmacological properties and the production of studies on the scaling of the synthesis of the most active substance, the development of methods for controlling its quality and stability research; methods - general methods of traditional and ultrasonic organic synthesis, UV, IR, PMR spectroscopy, chromatography (TLC, HPLC, LC / MS), virtual screening (PASS-online, docking research), statistical methods of data processing; novelty - the original methodology of scientific research, synthesized more than 300 new substances, anilides of 4,5-disubstituted (1,2,4-triasole (4H) -3-yl) thioglycolic acid, previously not described in the literature, for which the basic physical, physico-chemical characteristics and proven structure. For the first time, the strategy of synthesizing key intermediates has been chosen taking into account the possibility of further introduction into industrial production. For the first time systematic research and experimentally proved the feasibility of using ultrasound synthesis for a given number of compounds. According to the results of the previous in silico screening, the pharmacological activity of the synthesized substances was first planned and investigated for the purpose of the detection of antispasmodic, analgesic, anti-ulcer (in vivo) and anticancer (in vitro) properties. New patterns of dependence of the studied types of activity on the structure of synthesized substances, including using QSAR analysis, were revealed. The potential original antipsychotics - triazoprazole, for which the scaling of the laboratory method of synthesis has been investigated in the light of modern scientific approaches, has been determined, the original methods of quality control have been developed and the stability has been proved during storage for 1 year. Scientific novelty is confirmed by the patent of Ukraine for invention and 2 patents for utility model; results - developed preparative methods for the synthesis of substances that are readily reproducible and can be used for the synthesis of structural analogues, the library of 2,4-dihydro-3H-1,2,4-triazole-3-thione derivatives is added and their physical and spectral characteristics, revealed substances with a high level of anti-ulcer, analgesic and anticancer activity, prospects of further targeted synthesis of BAS in this direction; The method of triazoprosol synthesis was modified, taking into account the principles of "green chemistry", the scalable method of synthesis and methods of quality control of the "leader compound" - triazoprazole tested in the conditions of the industrial enterprise, synthesis of substance for in-depth research and pharmaceutical development of the pharmaceutical form was performed. The methods of determining the admixture of admixture and the quantitative content of triazoprosol have been developed. Preliminary data on the stability of the substance are obtained; implemented - in the scientific and pedagogical process of higher educational institutions, practice of pharmaceutical companies; branch - pharmacy.
