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Information × Registration Number 0224U033582, (0120U100310) , R & D reports Title Search, design and study of the action mechanisms of new biologically active compounds based on natural and synthetic scaffolds popup.stage_title Вивчення зв’язку між структурою і біоактивністю органічних сполук на основі природних і синтетичних скафолдів. Head Vovk Andrii I., Доктор хімічних наук Registration Date 31-12-2024 Organization V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry of the National Academy of Sciences of Ukraine popup.description1 Search, design and study the properties of new potentially bioactive heterocyclic and organophosphorus compounds directed to therapeutically important protein targets. popup.description2 As a result of the research, the search, design and properties of new biologically active heterocyclic and organophosphorus compounds based on natural and synthetic scaffolds were substantiated. In particular, it was found that new calix[4]arenes functionalized with sulfonamide, phosphonate or phosphate groups can inhibit some glutathione-S-transferases, phosphatases, malate dehydrogenase and acetylcholinesterase. The regularities of complexation of thiamine and thiazolium salts with albumin were established. The inhibitory effect of thiamine and its N-benzyl O-acyl-substituted structural analogues on the formation of amyloid structures of serum albumin was demonstrated. The directions of design of selective inhibitors of acetylcholinesterase or butyrylcholinesterase, the use of thiazolium derivatives for blocking membrane channels, as well as the use of thiazolium salts as potential neurotropic agents were substantiated. The properties of nitroxyl radicals with a resorcinarene scaffold in model liposomal systems were characterized by the EPR method. It was demonstrated that chalcone-4-carboxylic acid derivatives are capable of effectively inhibiting xanthine oxidase and exhibiting antioxidant properties. Regularities between the structure and activity of other related flavonoids - dihydrochalcones, Δ2,3-homoisoflavonoids, Δ3,9-homoisoflavonoids and their oxa-analogs were established. Effective xanthine oxidase inhibitors were searched and identified among furanylbenzoic acid derivatives with a pyrazolone or rhodanine fragment. The design of new xanthine oxidase inhibitors based on scaffold and bioisosteric substitutions in the drug molecule febuxostat has been performed. The design of α-glucosidase inhibitors based on hybrid compounds formed by azoles and flavonoids, including coumarins, chromones, isoflavones and aurones, has been substantiated. Product Description popup.authors Beiko Alona V. Buldenko Vladyslav M. Kobzar Oleksandr L. Muzychka Oksana V. Sukhovieiev Oleksandr V. Tanchuk Vsevolod Yu. Shulha Yurii V. popup.nrat_date 2024-12-31 Close