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Information × Registration Number 0221U105240, 0117U004134 , R & D reports Title Synthesis, structure, properties and molecular mechanisms of action of new antithrombotic and antiviral agents. popup.stage_title Head Andronati Sergii A., д.х.н. Registration Date 16-06-2021 Organization Physico-Chemical Institute O. Bogatsky National Academy of Sciences of Ukraine popup.description2  A number of 2-(piperazin-1-yl)quinazoline derivatives containing fluorine-containing -amino acid residues were synthesized. The synthesized quinazoline derivatives have been shown to inhibit platelet aggregation in vivo in the submicromolar concentration range. New indoloquinoxalines, indenoquinoxalinones and their oximes - potential immunomodulators, antiviral and anti-inflammatory agents - have been synthesized. Bromination of 7-methylindenoquinoxalinone with N-bromosuccinimide followed by aminodebromination synthesized 5 previously undescribed 7-aminomethyldeninoquinoxalinones. In a number of indenoquinoxalinones the ability to intercalate in DNA with affinity at the level of lgKd = 7 was shown for the first time. The formation of isomers of substituted indenoquinoxalinones and indoloquinoxalinones by condensation of asymmetric diaminobenzenes with ninhydrin and isatin, respectively, was investigated by the LC-MS method. For the synthesized compounds, the anti-inflammatory activity and the ability to induce interferon in vivo were studied. It has been shown that indoloquinoxalines at doses of 30 μmol / kg inhibit carrageenan edema in the paws of mice, and in the micromolar concentration range - induced synthesis of proinflammatory cytokines in vitro. For some indoloquinoxalines, the ability to induce interferon in vivo when administered orally has been shown. For oximes of indenoquinoxalinones, the ability to inhibit the activity of JNK protein kinases has been established. The correlation (P <0.007, R2 = 0.683) between the anti-inflammatory activity of isatin oximes and their lipophilicity was established. The GTM procedure was used to form and study the chemical space of various antiviral agents. Two-dimensional maps have been constructed on which compact zones of chemical space associated with various antiviral agents against viruses of different taxonomic groups (Enterovirus, Hepacivirus, Orthomyxoviridae, Lentivirus, Orthohepadnavirus, Pestivirus) Product Description popup.authors Illyushko Natalia О. Duma Hanna І. Kabanova Tetiana A. Karpenko Oleksandr S. Kornylov Oleksandr Yu. Krysko Andrii А. Kuzmin Viktor Ye. Lyakhov Sergii A. Mikhaylova Tetiana V. Shibinska Marina O. popup.nrat_date 2021-06-16 Close