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Information × Registration Number 0221U106621, 0121U109327 , R & D reports Title Synthesis of new derivatives of getaryl chalcones and trifluoromethyl-pyrroles and evaluation of their activity as inhibitors of therapeutically important enzymes popup.stage_title Head Sorochynskyi Oleksandr Ye., к.х.н. Registration Date 16-12-2021 Organization V.P. Kukhar Institute of Bioorganic Chemistry and Petrochemistry of the National Academy of Sciences of Ukraine popup.description2 The literature data on the synthesis of trifluoromethylpyrroles was generalized and systematized. N-(β-Polyfluoroacyl)vinyl derivatives of the proline, pipecolic acid and N-substituted glycines were synthesized by treatment of corresponding amino acids with β-alkoxyvinyl(polyfluoroalkyl) ketones. The cyclization of N-(β-trifluoroacyl)vinyl derivatives of cyclic amino acids in the presence of anhydrides and chlorides of organic acids has been systematically studied. The structures of cyclization products were established. Bicyclic trifluoromethylpyrroles were synthesized. A cyclization mechanism which explains the formation of bicyclic trifluoromethylpyrroles and bicyclic pyrroles containing trifluoromethyl and trifluoroacetyl groups in the pyrrole ring was proposed. Catalytic hydrogenation of bicyclic trifluoromethylpyrroles was investigated and trifluoromethylated derivatives of pyrrolizidine and indolizidine with define stereochemistry were obtained. Optimal conditions for the heterogeneous hydrogenation reactions using platinum, palladium and rhodium catalysts have been established. Computer simulations have shown that among trifluoromethylpyrrolidines, trifluoromethylpiperidines, and trifluoromethylpyrroles there are potential inhibitors of therapeutically important enzymes, such as cholinesterase, protein tyrosine phosphatase, xanthine oxidase, leucine-transupitase. Structural analogues of chalcones and getaryl chalcones as inhibitors of glutathione-S-transferase, PTP1B and xanthine oxidase have been studied in vitro. Product Description popup.authors Buldenko Vladyslav M. Gerus Ihor I. Klipkov Аnton А. Kobzar Olexandr L. Shaitanova Olena M. Shulga Yuriy V. popup.nrat_date 2021-12-16 Close