Work number - M 50 AWARDED
Author: Kaplaushenko A.G., Doctor of Pharmacy, Associate Professor
Presented by Zaporozhye State Medical University
In this work we solve the most important scientific problem of Medicine and Pharmacy, namely based on targeted synthesis of more than 350 compounds among 4-mono-and 4,5-disubstituted 1,2,4-triazole-3-thiones, the study of their biological activity, the potential original low-toxic neuroprotective drug with adaptogenic properties, namely "TIOMETRIZOL" has been developed. This drug has antioxidant and anti-ischemic mechanism of action. Prevention, first aid and treatment of diseases associated with cerebral ischemia, as well as for increasing the adaptive capacities of the organism have been scientifically proven for this drug.
Scientific basis and methodology of synthesis as well as the study of the biological activity of new compounds, namely 4 mono-and 4,5-disubstituted 1,2,4-triazole-3-thiones, have been developed. Methods of quality control, laboratory synthesis procedure, projects of technical conditions regarding the final product and intermediates have been received. Technological regulations for obtaining the substance and dosage form of potential drug "TIOMETRIZOL” have been developed.
There were 320 previously unknown compounds, as well as the results of pharmacological screening, in which substances exceed the activity of known drugs, the establishment of regularity "structure - biological effect", studies of pharmacokinetics, determination of possible ways of potential drug biotransformation suggest about global level.
Scientific results are displayed in 85 major works, including 49 articles (including 2 foreign journals, two journals that are in bibliographic database, 40 scientific publications in Ukraine, of which 7 are single-author papers), 22 reports. Novelty and competitiveness is protected by14 patents, including 2 patents of Ukraine for invention patents and 12 for utility model. Total number of links in bibliographic databases on publications of the author is 15.
Total number of author’s publications is 196.