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Information × Registration Number 0318U004058, 0117U007285 , R & D reports Title Development of synthesis methods of original organic compounds - potential modulatоrs SIRT1 with antidiabetic properties popup.stage_title Розробка способів синтезу оригінальних органічних сполук - потенційних модуляторів SIRT1 з антидіабетичними властивостями Head Yaremenko Fedir Heorhiyovich, Кандидат хімічних наук Registration Date 21-02-2018 Organization State Institution "V. Danilevsky Institute for Endocrine Pathology Problems National Academy of Medical Sciences of Ukraine" popup.description2 The objects of the study were rats, mice, condensed and spiro- nitrogen-containing heterocyclic compounds. The purpose of the study is to develop the methods of synthesis and the proof of the structure of original organic compounds - derivatives of different classes of nitrogen-containing heterocycles, which are pharmacologically active ligands of SIRT1 for the subsequent creation on this basis of future innovative means of overcoming the metabolic syndrome, as well as associated cardiovascular and oncological diseases. Methods of research - organic synthesis, physical and chemical analysis, biochemical, pharmacological, molecular biological. Methods for the synthesis of 3-spiro [indole-3,2'-pyrrolidine] -3-spiro [indole-3,2'-pyrolizidine] -2-ones and the original benzodiazepine derivatives have been developed to further investigate their ability to act as SIRT1 modulators and to reveal anti-diabetic properties. Their structure and the degree of purity have been proved by spectral and chromatographic methods. Methods of synthesis in increased loads of the most active compound-modulators SIRT1 have been worked out. In experimental models of type 2 diabetes mellitus, accompanied by obesity, the specific antidiabetic effect of the two most promising compounds revealed in the previous stages in in vitro and in vivo experiments was studied. The study of the specific antidiabetic activity of two most promising compounds revealed in the previous stages in in vitro and in vivo experiments (Z1768420549 and EN300-183708) in type 2 diabetes mellitus caused by the introduction of streptozotocin on the base of high-carbohydrate diet in rats demonstrated their ability to reduce the parameters of disglycemia, insulin resistance, and blood pressure. The field of application - healthcare, pharmaceutical industry. Product Description popup.authors Бородіна В.В. Вакула В. М. Гладких О.І. Земляна Н. І. Карножицька Т. М. Кравченко С.В. Красова Н.С. Лещенко Ж. А. Лукацька Л. Л. Полторак В.В. Свидло І.М. Сова О. М. Тижненко Т. В. Устенко Н. В. Яременко Ф.Г. popup.nrat_date 2020-04-02 Close