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Synthesis, characterization, cytotoxicity and antibacterial activity of salicylaldehyde based aroylhydrazones

Hydrazones, represented by the general formula R1R 2C=N–NR3R 4 , are used in the synthesis of heterocyclic compounds, drug design, organocatalysis and coordination chemistry.[1, 2] These compounds exhibit interesting biological applications, such as anti- inflammatory, analgesic, antiplatelet, anticonvulsant, antitumoral, antiviral and antimicrobial activity.[1] The presented research is focused on the synthesis, characterization and biological activities of the selected aroylhydrazones. The condensation of salicylaldehyde derivative, namely 3- or 4- hydroxysalicylaldehyde, and hydrazide, specifically nicotinoyl- or isonicotinoylhydrazide, was achieved by conventional synthetic method (i.e. in the solution) as well as by the solventfree mechanochemical procedure. The synthesized compounds were characterized by the elemental and DSC analysis, IR and NMR spectroscopy. The molecular and crystal structures were determined by the single-crystal X-ray diffraction method. The in vitro cytotoxicity of hydrazones was investigated against THP-1 and HepG2 cells. Each cell line was treated with various concentrations of the tested compounds and the viability of cells after treatment was determined using MTS assay. Half maximal inhibitory concentration (IC50) values were calculated from dose‐response curves. Hydrazones were also tested for their in vitro antimicrobial activity against Gram-positive (Staphylococcus aureus and Enterococcus faecalis) and Gramnegative (Escherichia coli and Moraxella catarrhalis) bacteria by broth microdilution method. The results are reported in minimum inhibitory concentration (MIC) values.

hydrazones ; citotoxicity ; antibacterial activity

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