Registration Number
0217U003648,
0114U000968
, R & D reports
Title
Targeted search of biologically active compounds among substituted triazinoquinazoines and development of candidates for drugs based on them.
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Head
Kovalenko Sergiy Ivanovych, Доктор фармацевтичних наук
Registration Date
14-06-2017
Organization
Zaporozhye State Medical University
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Presented scientific work is devoted to the purposeful search of biologically active agents among substances containing triazinoquinazoline fragment. It is found, that substituted 3-R-[1,2,4]triazino[2,3-c]quinazolin-2-ones while reaction with excess of hydrazine hydrate in propanol-2 yielded the corresponding 3-(2-amino-3-R1-4-R2-5-R3-phenyl)-6-R-1,2,4-triazin-5 (2H)-ones. It is shown, that 3-(2-amino-3-R1-4-R2-5-R3-phenyl)-6-R-1,2,4-triazin-5(2H) -ones are classical binucleophilic agents, and may act as starting compounds for the formation of combinatorial libraries of substituted triazinoquinazolines. The interaction of 3-(2-amino-3-R1-4-R2-5-R3-phenyl)-6-R-1,2,4-triazin-5(2H)-ones with carbonyl compounds, acylating reagents, carbon disulfide, potassium xanthate, carbonyldiimidazole, nitrous acid, isocyanates, isothiocyanates, compounds with activated triple bond, etc. It is established, that products of substituted 3-(2-amino-3-R1-4-R2-5-R3-phenyl)-6-R-1,2,4-triazin-5(2H)-ones modification exhibit versatile biological action in particular anticancer, antimicrobial, antifungal, antioxidant, antihypoxic, anti-ischemic and actoprotective. Sodium 4-(3-methyl-2-oxo-2H-[1,2,4]triazino[2,3-c]quinazolin-6-yl)butanoate is proposed for further pharmacological studies as promising anti-ischemic agent.
Product Description
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Берест Галина Григорівна
Воскобойнік Олексій Юрійович
Коломоєць Олександра Сергіївна
Кривошей Оксана Вікторівна
Носуленко Інна Степанівна
Синяк Раїса Степанівна
Скорина Дмитро Юрійович
Ставицький Віктор Валерійович.
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2020-04-02