Amidrazones and their derivatives are known for a wide spectrum of biological effects: antifungal, antibacterial, anti-inflammatory, antithrombotic and antitumor activity. The aim of the studies was to obtain new biologically active substances.

Three hydrazide derivatives (1-3) were synthesized in reaction of N³-substituted amidrazones with itaconik anhydride in anhydrous ether. Their structures were determined by nuclear magnetic resonance spectroscopy. Potential biological effects of novel compounds were predicted with PASS (Prediction Activity Spectra for Substances) software. According to PASS calculations hydrazides (1-3) could develop anti-inflammatory activity. 

Hydrazides (1-3) were studied for their ability to affect cytokines (IL-6 and TNF-α) production in human whole blood cultures to determine their anti-inflammatory effect. Both chosen cytokines are important inflammatory mediators. Compounds were used in concentrations 0,1µg/mL, 1µg/mL and 10µg/mL. The cell cultures were stimulated with lipopolisaccharide (LPS) to produce IL-6 and TNF-α. The activities of cytokines were measured in the supernatants using bioassays.

The results indicate that TNF-α production was slightly reduced (about 10%) by compounds 1 and 3 in concentration 1µg/mL. However the same compounds in concentration 10µg/mL caused stronger inhibition: 57% and 23%, respectively. Derivative 1 did not affect production of IL-6, while hydrazide 3 increased this cytokine production. Compound 2 showed no TNF-α or IL-6 inhibition.

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