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Information × Registration Number 0219U102407, 0115U002587 , R & D reports Title The synthesis of novel bioactive derivatives of azaheterocycles and study of their properties. popup.stage_title Head Brovaretz Volodymyr S., Доктор хімічних наук Registration Date 28-12-2019 Organization V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry of the National Academy of Sciences of Ukraine popup.description2 In order to search for biologically active compounds, the interaction of the available 1-acylamino-2,2-dichloroacrylic acids with N-methyl-D-glucamine is investigated. It’s been shown that the interaction of 1-acylamino-2,2-dichloroacrylonitriles and diethyl ester of 1-acylamino-2,2,2-trichloroethylphosphonic acids with the natural alkaloid cytisine leads to compounds with pharmacophore 1,3-oxazole fragment. 5-Morpholino-1,3-oxazole-4-carbonitriles, which contain in position 2 of the oxazole ring 4-phthalimidobutyl or 5-phthalimidopentyl substituent, were synthesized. Preparative approaches to obtain previously unknown methyl esters of 2-aryl-5-chlorosulfonyl-1,3-oxazole-4-carboxylic acids have been developed. It’s been founded that the interaction of 7-phenyl-3H,4H,7H-pyrazolo[3,4-d]-1,2,3-triazine-4-one with alkyl halides and formaldehyde proceeds with the preservation of the pyrazolotriazine structure. Preparative approaches to the synthesis of pyrazoloacetic acids containing pharmacophore arylthio- and arylsulfonyl groups have been developed. A general approach to the synthesis of 1,3-thiazole derivatives containing hydroxyalkyl groups at the 2 and 5 ring positions is proposed. Substituted 2-hydroxyalkyl-1,3-thiazole-5-carbaldehydes and 5-hydroxyalkyl-1,3-thiazole-2-carbaldehydes were reacted with phenylhydrazine, isoniazid, N-substituted rhodanines, and the Biginelli reaction. Previously unknown 4-amino-5-methylsulfonylpyrimidines and their condensed derivatives were obtained, some of the derivatives were investigated in vitro against poliovirus type 3 (PV-3). 4-Cyano-1,3-oxazole-5-thiols, 2-substituted 5-arylsulfonyl-1,3-oxazole-4-carbonitriles and 7-piperazinesubstituted 1,3-oxazole[4,5-d]pyrimidines were synthesized and investigated on anticancer activity against a group of 60 cancer cells at the National Cancer Institute, USA. Product Description popup.authors Іvanova Іryna V. Abdurakhmanova Esma R. Biletska Іryna M. Veligina Yevheniia S. Vydzhak Roman M. Golovchenko Оleksandr V. Hurenko Artem O. Didiv Nataliya D. Demydchuk Bogdan A. Zhirnov Viktor V. Zyabrev Volodymyr S. Kachaeva Maryna V. Kachkovskyi Oleksiy D. Кlyuchko Svitlana V. Kozachenko Olexandr P. Kondratyuk Kostyantyn M. Mityukhin Оleg P. Merzhievskiy Danylo O. Moskvina Viktoria S. Mrug Galyna P. Pilyo Stepan G. Panchyshyn Svitlana Ya. Polovko Тetiana A. Popova Antonina V. Porhun Svitlana V. Prokopenko Volodumir M. Prostota Yaroslav A. Rentsevych Тetiana L. Synenko Vitaliy O. Slyvchuk Serhiy R. Solomyanyi Roman M. Turov Кostyantyn V. Frasinyuk Mykhaylo S. Charochkina Larysa L. Chumachenko Svitlana A. Shablykin Оleg V. Shablykina Olga V. Iakovenko Іgor N. popup.nrat_date 2020-04-02 Close