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Information × Registration Number 0223U005817, 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 Head Vovk Andrii I., Доктор хімічних наук Registration Date 31-12-2023 Organization V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry of the National Academy of Sciences of Ukraine popup.description2 As a result of the research, new pyrazolone-containing xanthine oxidase inhibitors with a furan-2-ylbenzoic acid scaffold were identified. The mechanisms of the enzyme inhibition were clarified and the dependence of the inhibitory effect of the investigated compounds in the presence of albumin in vitro was established. Mechanisms of xanthine oxidase inhibition by pyrazolone-containing derivatives of 3-(hydrazinyl)- and 4-(hydrazinyl)benzoic acid were investigated using a molecular dynamic method. The study results of the inhibitory activity against nucleotide pyrophosphatase/phosphodiesterase 1 of synthesized 6-substituted derivatives of purine and its heterocyclic isosteres (pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine) are presented. ADMET parameters were evaluated and the in vitro effect of new derivatives of calix[4]arenes on the activity of several therapeutically important enzymes was investigated. It was found that tetrakis-substituted calix[4]arenes with N-carbamoylbenzenesulfonamide and thioxotetrahydropyrimidine substituents on the upper rim can be effective and selective inhibitors of glutathione S-transferases. The obtained results are important for the search and creation of new inhibitors of purine metabolism, as well as new regulators of biochemical processes involving nucleotide pyrophosphatases and glutathione S-transferases. Product Description popup.authors Buldenko Vladyslav M. Hushcha Tatiana О. Kobzar Oleksandr L. Mischenko Iryna M. Mykula Mariya S. Muzychka Oxana V. Sukhoveev Olexandr V. Tanchuk Vsevolod Yu. Tatarchuk Alʹona V. Yrij V. Shulga popup.nrat_date 2023-12-31 Close