A series of hydrazones based on hydrazides of o-and p-hydroxybenzoic acids have been prepared. N-(5-Bromo-2-hydroxybenzylidene)-4-hydroxybenzohydrazide has been studied by X-ray diffraction analysis; its molecule forms hydrogen bond with a solvating ethanol molecule. Biological activity of the synthesized hydrazones towards cathepsin Е and(or) elastase of human neutrophils has been determined.
The article presents the results of a study by the authors of the article on the development of new ways of synthesis and study of the biological activity of hydrazide derivatives of o-hydroxybenzoic acid. Methods for the preparation of hydrazone, oxadiazole, thiosemicarbazide, 1,2,4-triazole-3-thionic derivatives and methods for their further modification are described. The condensation reaction of hydroxybenzoic acid hydrazides with 1-deoxy-2,3,4,6-tetra-O-acetyl-D-glucopyranosyl isothiocyanate synthesized their corresponding acetylated glycosyl-contai-ning thiosemicarbazide derivatives. The structures of the synthesized compounds were studied by 1H and 13C NMR spectroscopy, as well as by the data of two-dimensional spectra of COSY (1H-1H) and HMQC (1H-13C). The values of chemical shifts, multiplicity, and integrated intensity of 1H and 13C signals in one-dimensional NMR spectra were determined. Using spectra in the formats COSY (1Н-1Н) and HMQC (1Н-13С), homo- and heteronuclear interactions were established, confirming the structure of the compounds under study. The results of evaluating their antimicrobial, anti-inflammatory and cytotoxic activity (in vitro) on cultures of human monocytic cell lines MonoMac-6 and THP-1Blue are described.
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