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Information × Registration Number 0224U000181, 0121U107777 , R & D reports Title Development of promising methods for designing compounds with antimicrobial and anticancer action popup.stage_title Head Pokhodylo Nazarii T., Доктор хімічних наук Registration Date 03-01-2024 Organization Ivan Franko National University of Lviv popup.description2  Research object: Heterocyclizations, tandem reactions, domino reactions, cycloaddition, synthesis of biologically active substances, antimicrobial activity, anticancer activity, apoptosis. The purpose of the work is the development of new variants of one-pot, multicomponent, tandem and domino reactions based on organic 1,3-dipoles (azides, diazo compounds, oxonitriles, nitrilimines), synthesis of drug-like substances for screening for biological activity, research of their antimicrobial and antitumor activity and study of cellular mechanisms of their action. Research methods: Organic synthesis, elemental analysis, spectral methods (IR, 1H NMR and 13C spectroscopy, mass spectrometry), chromatography and X-ray structural analysis. In silico research methods include DFT calculations, molecular mechanics, Hirschfeld surface analysis, virtual screening, COMPARE analysis and docking studies. Methods of biochemical, microbiological research and cell biology. Obtained results. As a result of the conducted research, effective and resource-saving approaches to the synthesis of compound libraries of 1H-1,2,3-triazole, tetrazole, and 1,2,4-oxadiazole derivatives were developed, which were evaluated for their antimicrobial activity and antitumor effect. New conjugates of 1,2,3-triazole and thienopyrimidine containing natural or related compounds were synthesized. Techniques including tandem and domino reactions have been developed. Derivatives of polycyclic systems [1,2,3]triazolo[1,5-a]pyrazine, 2-(triazol-4-yl)-thieno[2,3-d]pyrimidine and thieno[3,2-e][ 1,2,3]triazolo[1,5-a]pyrimidine. Reactions of thermally activated transannelation of 1H-tetrazoles were studied. The drug-likeness parameters of the compounds were evaluated. Compounds that inhibit the growth of cancer cells in nanomolar concentrations were discovered, and the molecular and cellular mechanisms of their action were studied. Compounds showing high activity against methicillin-resistant Staphylococcus aureus were Product Description popup.authors Manko Nazar Olegovych Pitkovych Khrystyna Yevhenivna Tupychak Mykola Anatoliyovych Finiuk Nataliya Stepanivna popup.nrat_date 2024-01-03 Close