Registration Number
0220U100550,
0115U002770
, R & D reports
Title
Molecular design of bioactive systems based on functionalized azoles.
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Head
Bratenko Mykhailo K., Доктор хімічних наук
Registration Date
21-01-2020
Organization
HSEE of Ukraine "Bukovinian State Medical University"
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This works deals with elaboration of the method of synthesis of new chemotypes of the functionalized azoles from the series of 4-chloro-1H-imidazoles and with their targeted structural modification for further construction of new bioactive systems. As a result, some representatives of (imidazole-5-il)hydrazones and thiosemicarbazones, 1-nitro-2-(imidazole-5-il)ethenes, 4-(imidazole-5-il)-2-oxo-1,2-dihydropyridine-3-carbonitriles and the imidazole-containing 2-amino-4H-chromenones, exhibiting a wide spectrum of antimicrobial activity within concentrations 0.25-125 μg/ml were identified. It has been found that the efficiency of some representatives of N'-[(1Н-imidazole-5-il)methylene]isonicotinhydrazides, thiosemicarbazones of 5-formyl-4-chloro-1Н-imidazoles and 1-aryl-5-trifluoromethyl-4-chloro-1Н-imidazoles against М. tuberculosis in concentration of 0.05 μg/ml is 4 times better than that of the first row medicine isoniazid while the acute toxicity of the former compounds remains much lower. The in vitro experimental results prove that the 5-carbofunctionalized derivatives of imidazole-4-thioalkanecarbonic acids exhibit an explicit antioxidant activity when applied within the concentrations 10-1-10-3 mole/l while some representatives prove even higher efficiency than that of the reference medicine thiotriazoline. The in vivo investigation of hypoglycemic activity of {5-[(1,3-thioazolidine-5-iliden)methyl]imidazole-4-il}thioacetic acids, 5-[(1-aryl-4-chloro-1Н-imidazole-5-il)methylene]-1,3-thioazolidine-2,4-diones and their exohydrated analogs proved that their hypoglycemic effect was deeper and more prolonged than that of the reference medicine pioglitazone while the acute toxicity of the former compounds was lower. This result allows us to preclassify these compounds as a new prospective class of the hypoglycemically active agents.
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Barus Marianna M.
Bratenko Mykhailo K.
Burdenyuk Ivan Pavlovich
Velyka Alla Ya.
Havrylyuk Olesya I.
Hrozav Alina M.
Deyneka Svyatoslav Ye.
Panasenko Nadiia V.
Perepelitsa Olesya O.
Rotar Diana V.
Svijak Veronika K.
Chornous Vitaliy O.
Yakovichuk Nina D.
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2020-04-02
