Sakharova T. Experimental study of pharmacodynamic and mechanism of action of new group natural antioxidants on a basis ellagotannins

The dissertation is devoted to pharmacognostical studies of vegetative and generative parts of Ukrainian Milk thistle. Qualitative composition and quantitative content of different groups of biologically active substances in plant raw material and obtained lipophilic fractions was studied. The 26 individual substances have been isolated from roots and grass of Milk thistle and their structure was determined; 15 amino acids and 22 microelements were found out. The content of 11 fatty acids, chlorophylls and carotinoids was determined in obtained fractions. The drafts of Analytical Normative documentation were developed on "Milk thisle's grass", "Milk thisle's roots", "Milk thistle's fruits", "Milk thistle's oil" and "Species against diabetes mellitus". Hepatoprotective, antioxidant, immunostimulative action of Milk thistle's oil and fruits was studied. New species against diabetes mellitus was developed using Milk thistle's fruits. 1,8,8-trimethyl-3-(4-оxо-2-alkyl(aryl)-3,4-dihydroquinazolin-3-il)-3-azabicyclo[3.2.1]-octan-2,4-diones has been determined. For the first time the method of formation quinazolin-4(3H)-ones by the reaction anthranilamide with ?-diketones has been discovered. The hypoglycemic, diuretic, antimicrobic, anticoagulatic, hemostatic, anticonvulsive screening of the synthesized compounds has been conducted. The "structure - activity" relationship for these types of activities have been determined. According to the results of biological assay two low-toxic substances 3-[2-(2-(5-bromothiophene-2-yl)-2-oxoеthylthio)-4-oxo-3,4-dihydroquin-azo-lin-3-yl]-1,8,8-tri-me-thyl-3-azabicyclo[3.2.1]octan-2,4-dione (with hipoglicemic activity) and 3-[2-(2-(3-nitrophenyl)-2-oxoеthylthio)-4-oxo-3,4-dihydroquin-azo-lin-3-yl]-1,8,8-tri-me-thyl-3-azabicyclo[3.2.1]octan-2,4-dione (with high anticonvulsive activity) has been recommended for profound pharmacological study.