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Information × Registration Number 0214U008148, 0109U004375 , R & D reports Title Search of new pharmacological means on a basis nitrogen - and sulphurcontaining heterocycles. popup.stage_title Head Kharchenko Aleksandr Vasilievich, Доктор хімічних наук Registration Date 05-09-2014 Organization State higher educational entity "Ukrainian State University of Chemical Technology" popup.description2 Research object: pyrrol-5-yl urea, Curtius rearrangement, antioxidant, anticonvulsant, analgesic activity. Objective: Synthesis of new N-substituted N'-(2,4-dimethyl-3-carbethoxy) pyrrol-5-yl ureas and research of their antioxidant, anticonvulsant, analgesic activity in vitro. Research methods: organic synthesis, biological tests, thin layer chromatography, IR-, NMR-, and MASS-spectroscopy. Produced preparative method of synthesis of ethyl 5-amino-[(hydrazinocarbonyl)amino]-2,4-dimethyl-1H-pyrrole-3-carbonoate and ethyl 5-aminocarbonyl-2,4-dimethyl-1H-pyrrole-3-carbonoate by not continious deflux of 5-azidocarbonyl-2,4-dimethylpyrrol-3-carbonoate in dioxane with an aqueous solution of ammonia or hydrazine hydrate in resalt of the reserch work. Under these conditions the synthesis of N-substituted N'-(2,4-dimethyl-3-carbethoxy) pyrrol-5-yl ureas for pharmacological screening for antioxidant activity was made. Pharmacological screening demonstrate enhanced antioxidant activity of pyrrole-5-yl urea derivatives in oxidative protein modification under conditions of initiation of free radical oxidation in vitro. These derivatives prevent accumulation of the products of oxidative modification. Studied preparative procedure for the synthesis of ethyl 5-carbomoylamino-2,4-dimethyl-1H-pyrrole-3-carboxylic acid and 3,5-dikarbomoylamino-2,4-dimethyl-1H-pyrrole by short boiling of the corresponding ethyl ester 5-azidocarbonyl-2,4-dimethylpyrrol-3-carboxylic acid or 3,5-diazidocarbonyl-2,4-dimethylpyrrol in dioxane with an aqueous ammonia solution. In the same conditions obtained N- substituted N'-(2,4-dimethyl-3-carbethoxy)pyrrol-5-yl ureas and 2,4-dimethyl-3,5-dicarbomoylaminopyrroles for pharmacologic screening. Biological tests demonsterate that new pyrrolyl urea derivatives exhibit analgesic and anticonvulsant activity. Application area: С 21.10 Manufacture of basic pharmaceutical products. Product Description popup.authors Астахіна Валерія Олегівна Білов Володимір Вітальович Бойко Сергій Романовіч Воєвудський Максим Вадимович Карпіщенко Людмила Сергіївна Кисельов Вадим Витальович Крищік Оксана Володимірівна Марков Віктор Іванович Нічволода Віктор Михайлович Парамонова Тетяна Грігоріївна Харченко Олександр Васильович Чорноус Станислав Юрійович Якименко Ігор Юрійович Янова Кароліна Валентинівна popup.nrat_date 2020-04-02 Close