R&D registration number in UkrISTEI: 0117U004134
What priority area of science and technology does it correspond to: fundamental scientific research on the most important problems of developing scientific, technical, socio-economic, socio-political, human potential to ensure the competitiveness of Ukraine in the world and the sustainable development of society and the state
Research: fundamental
Funding source: state budget; general fund of the state budget
The amount of financing: more than 1000 thousand UAH. (1255.578 thousand UAH).
The total duration of the study (according to the plan): 2017-2021.
Prospect for further implementation in 2022-2023: to be completed.
Research level: no analogues in the world
Patent: no
Additional activities requiring further research: modern scientific equipment; search for interested investors
Brief description, advantages, further prospects for application.
The work is devoted to the synthesis and study of the biological activity of new antagonists to the “closed form” of fibrinogen receptors, potential antiviral agents, interferon inducers, DNA ligands and anti-inflammatory agents. study of the influence of structure on biological properties
A targeted synthesis of 2-(homopiperazin-1-yl)quinazolin-4-one derivatives was carried out. It has been shown that derivatives of 2,6-substituted quinazolin-4-one inhibit the binding of fibrinogen to αIIbβ3 and their antiaggregation properties have been studied. The main binding sites of 2-(piperazin-1-yl)quinazoline derivatives to αIIbβ3 were determined by molecular docking.
Synthesized 9-R-6-H-indolo[3,2-b]quinoxalines starting from substituted isatins, as well as water-soluble analogues. The corresponding naphthalimide derivatives were synthesized by condensation of 6-unsubstituted and 6-bromono-petroleum anhydride with ammonia, hydrazine hydrate, and hydroxylamine. New derivatives of indenoquinoxaline were synthesized by condensation of ninhydrin with substituted 1,2-diaminobenzenes, from the latter the corresponding oximes were synthesized. The condensation of isatin with isatoic anhydride yielded tritantrines, and from them the corresponding oximes. It has been shown that indenoquinoxalinones are DNA intercalators. Indenoquinoxalines, indolo[2,1-b]quinazoline-6,12-diones and their oximes were studied for their ability to inhibit the induced production of pro-inflammatory cytokines and to inhibit the development of caraginan-induced edema. Active in vitro at micromolar concentrations and active in vivo at a dose of 34 µmol/kg of the compound were found.
The GTM procedure was applied to form and study the chemical space of various antiviral agents. As a result, two-dimensional maps were constructed, on which it is possible to identify compact zones of the chemical space associated with various antiviral agents in relation to viruses of various taxonomic groups (Enterovirus, Hepacivirus, Orthomyxoviridae, Lentivirus, Orthohepadnavirus, Pestivirus, Herpesvirus).