In recent decades, the efforts of many researchers in the sphere of organic chemistry, physics and pharmacol-ogy have been focused on the search for new agents with pronounced antibacterial and especially antifungal activity. This is due to the widespread increase in the resistance of many bacterial strains and fungi to antibi-otics and antifungal drugs available in medical practice. In this regard, the number of works related to the synthesis of new potential antibiotics from the most diverse class of organic derivatives, which either include known pharmacophore groups or represent a new structural class of compounds with unknown and unex-plored activity, is increasing in the scientific literature. In this work, new previously undescribed hydrazones derivatives were obtained on the basis of physiologically active isonicotinic and salicylic acid hydroxides and laboratory-available acetyl-substituted heterocycles, namely 3-acetyl-2H-chromen-2-one 3, 2-acetyl-3H-benzo[f]chromen-3-one 4 and 2,6-methanobenzo[g][1,3,5]oxadiazocine 5. The obtained hydrazones structure is explicitly proved by IR and 1H, 13C NMR spectroscopy data. The synthesized six new hydrazones under-went biological screening for antibacterial and antifungal activity on strains of microorganisms, namely gram-positive bacterium Staphylococcus aureus 209P, gram-negative bacterium Pectobacterium carotovorum VKM-B1247, and yeast-like fungus Candida albicans ATCC 10231. Screening revealed three compounds with antimicrobial activity and one promising compound — (E)-2-hydroxy-N’-(1-(2-oxochroman-3-yl)ethylidene)benzohydrazide 9, which also exhibits antifungal activity along with antimicrobial activity.
Production of cyclodextrin nanocomplexes based on N'-((5-nitrofuran-2-yl)methylene)isonicotinohydrazide and research of their structure by physical and chemical methods In the present work, the supramolecular complexes of N'-((5-nitrofuran-2-yl)methylene)isonicotinohydrazide with β-cyclodextrin (β-CD) and 2-hydroxypropyl-β-cyclodextrin (2-HP-β-CD)were first obtained and studied. The NMR methods of one-dimensional 1 H, 13 C spectroscopy confirmed the structure of the obtained inclusion complexes. The structure of the compounds was also studied by two-dimensional NMR spectroscopy COSY (1 H-1 H) and HMQC (1 H-13 C), which allows one to establish spin-spin interactions of a homo-and heteronuclear nature. Comparison of the integral intensities of the 1 H NMR signals of the initial substrate and βand 2-HPβ-CD in supramolecular complexes showed that in both cases complexes of the composition of one substrate molecule per one receptor molecule are formed. It was found that the interaction of N'-((5-nitrofuran-2-yl)methylene)isonicotinohydrazide with the studied β-cyclodextrins forms inclusion complexes with the penetration of the substrate molecule into the internal cavity of the receptor by the pyridine fragment in the case of using β-CD and the furanose cycle in the case of 2-HP-β-CD. The resulting supramolecular complexes can dissolve in water or form stable aqueous dispersions.
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