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Information × Registration Number 0215U000743, 0112U005998 , R & D reports Title Design and synthesis of novel targeted JNK kinase inhibitors and study of their insulinomimetichnoi and antiatherosclerotic activity popup.stage_title Head Kovalenko Sergey Mikolajovith, Registration Date 07-04-2015 Organization Nation University of Pharmacy popup.description2 Objective: Design, synthesis of selective inhibitors of reverse-Jun N-terminal kinases and their research in order to identify substances that exhibit insulinomimetychnu and antiatherosclerotic activity. A study was conducted to find new pharmaceutical substances as potential inhibitors of JNK-kinase. Methods: pharmacological, biochemical, physiological, physical, chemical and instrumental methods of mathematical statistics. Results: Calculations on optimization of the basic structures and the ways purposeful synthesis of predicted compounds. Synthesized 40 new compounds from substituted 4-N- (aryl) alkyl quinazoline and 10 new compounds - target amides of 2-amino-3-cyanothiophen. Studied the physicochemical properties of the synthesized compounds (solubility, melting point), using the ACD / Labs evaluated some physicochemical and molecular descriptors. Research invitro in isolated hepatocytes, the influence of these substances on the activity of alanine aminotransferase (ALT) in the incubation medium of hepatocytes and influence the content 3-acylghlyceryds and the influence of these substances on the activity of marker enzymes and lipid metabolism. Studied the activity of these compounds in conditions in vivo in experimental models of diabetes mellitus type 2 (DM2) in animals. The synthesized compounds do not exhibit hypoglycemic, hypolipidomic and antioxidant properties at a separate type, but provide an influence on the activation of JNK background and reduce its activation. The data confirm the applicability of selected compounds in complex protection under conditions involving the activation of JNK5481 Product Description popup.authors Євсєєва Лариса Валентінівна Вепрецька Людмила Володимирівна Грищенко Ірина Володимирівна Губарь Світлана Миколаївна Друшляк Олександр Григорович Загайко Андрій Леонідович Капустянський Ігор Юрієвич Коваленко Сергій Миколайович Красільнікова Оксана Анатоліївна Филимоненко Вікторія Павлівна Шевченко Світлана Макарівна popup.nrat_date 2020-04-02 Close