Registration Number
0226U003584,
(0122U000657)
, R & D reports
Title
Design, synthesis and structural-functional research of new antiplatelet agents and tetracyclic systems as antiviral, anti-inflammatory agents
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Молекулярний дизайн та синтез нових похідних 2-аміно-3H-хіназолін-4-ону, що містять у другому положенні хіназолінового гетероциклу піперазиновий, гомопіперазиновий або 2,5-діазабіцикло[2.2.1]гептановий фрагменти. Вивчання антиагрегаційної активності. Синтез похідних нафталіміду, що містять замісники у ароматичному ядрі, як потенційних противірусних агентів. Синтез оксимів інденохіноксалінону. Вивчення противірусної активності та афінітету до ДНК цільових сполук.
Head
Kuzmin Victor Ye., Доктор хімічних наук
Registration Date
20-04-2026
Organization
Physico-Chemical Institute O. Bogatsky National Academy of Sciences of Ukraine
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Directed design and synthesis of potential antagonists of fibrinogen receptors, DNA ligands and JNK inhibitors, study of functional biological activity of target compounds and establishing the connection "structure - properties - molecular mechanism of action".
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The purpose of the research: Directed design and synthesis of potential fibrinogen receptor antagonists, DNA ligands and JNK inhibitors, study of functional biological activity of target compounds and establishment of the "structure - properties - molecular mechanism of action" relationship.
The directed synthesis of 2-(piperazin-1-yl)quinazolin-4-one, 2-(homopiperazin-1-yl)quinazolin-4-one and 2-(2,5-diazabicyclo[2.2.1]heptan-2-yl)quinazolin-4-one derivatives was carried out. It was shown that the studied 2,6-substituted quinazolin-4-one derivatives inhibit the binding of fibrinogen to αIIbβ3 with IC50 values from 33 μM to 0.1 μM. The antiaggregatory properties of the synthesized 3H-quinazolin-4-one derivatives were also studied and it was found that the IC50 values are in the range from 62 μM to 0.04 μM. According to the previously developed method, 7- and 9-(dialkylaminoalkyl)amino triptanthrines were prepared - potential DNA intercalators and antiviral agents, and at the same time - precursors for the synthesis of potential anti-inflammatory drugs. The methods for the synthesis of 8-hydroxy and 8-aminotriptanthrine - convenient precursors for the synthesis of water-soluble triptanthrine derivatives - potential therapeutic agents - were optimized. Starting from N-(4-hydroxyphenyl)acetamide, 7(8)-(dialkylaminoethoxy)indenoquinoxalinones were synthesized in the form of a regioisomeric mixture. Separation of the mixture and establishment of the absolute configuration of the products are ongoing. The affinity of the synthesized compounds to DNA was studied by fluorimetric titration. All the studied compounds belong to intercalators of moderate strength.
Product Description
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Krysko Andrii А.
Karpenko Oleksandr S.
Kornilov Oleksandr Yu.
Duma Hanna І.
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2026-04-20
