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Amidrazones are known for the broad biological activity of their derivatives (antimicrobial, anti-inflammatory, antiparasitic, antitumor and others). While searching for new drugs, twelve new derivatives of N3-substituted amidrazones were obtained in the reaction with cis-1,2,3,6-tetrahydrophthalic anhydride. The structures of obtained linear compounds and 1,2,4-triazole derivatives were confirmed by 1H NMR, 13C NMR and MS. Toxicity and inflammatory activity of obtained compounds (at concentrations of 10, 50 and 100 µg/mL) were studied in human peripheral blood mononuclear cells (PBMC). The influence of new derivatives on cytokine production (TNF-α, IL-6 and IL-10) was examined in PBMC cultures stimulated by LPS. Antiproliferative activity of compounds was studied in PBMC cultures stimulated by phytohaemagglutinin. Minimal inhibitory activity of compounds was studied by broth microdilution method on Gram-positive (S. aureus, M. smegmatis) and Gram-negative (E. coli, Y. enterocolitica, K. pneumonia) bacterial and fungal C. albicans strain. Obtained 1,2,4-triazole derivatives were not toxic to PBMC at a concentration range of 10–100 µg/mL. Only one 1,2,4-triazole derivative showed significant antiproliferative activity at the highest dose. Five 1,2,4-triazole derivatives showed significant, stronger than ibuprofen, inhibition of pro-inflammatory TNF-α production at concentrations 10 and 50 µg/mL, as well as significant elevation of levels of anti-inflammatory cytokine IL-10 at each used dose. Two linear compounds showed antibacterial activity against Gram-positive bacteria. In conclusion, five obtained compounds showed a strong anti-inflammatory effect and deserve further research.

Amidrazones are widely used in chemical synthesis, industry and agriculture. We compiled some of the most important findings on the biological activities of amidrazones described in the years 2010–2022. The data were obtained using the ScienceDirect, Reaxys and Google Scholar search engines with keywords (amidrazone, carbohydrazonamide, carboximidohydrazide, aminoguanidine) and structure strategies. Compounds with significant biological activities were included in the review. The described structures derived from amidrazones include: amidrazone derivatives; aminoguanidine derivatives; complexes obtained using amidrazones as ligands; and some cyclic compounds obtained from amidrazones and/or containing an amidrazone moiety in their structures. This review includes chapters based on compound activities, including: tuberculostatic, antibacterial, antifungal, antiparasitic, antiviral, anti-inflammatory, cytoprotective, and antitumor compounds, as well as furin and acetylocholinesterase inhibitors. Detailed information on the compounds tested in vivo, along the mechanisms of action and toxicity of the selected amidrazone derivatives, are described. We describe examples of compounds that have a chance of becoming drugs due to promising preclinical or clinical research, as well as old drugs with new therapeutic targets (repositioning) which have the potential to be used in the treatment of other diseases. The described examples prove that amidrazone derivatives are a potential source of new therapeutic substances and deserve further research.

Introduction. Hormonal contraception could activate wide range of biological effects in women body and what’s important these pharmaceuticals are often used for long time. The aim of this study was to examine the level of knowledge among young women studying on the universities of Bydgoszcz (Poland) about the health effects of hormonal contraception. Materials and Methods. 172 women aged from 18 to over 25 years (the majority of respondents were in the age 21-24 years) were assessed with original anonymous questionnaire. Results. The state of knowledge of young women concerning negative aspects of using contraception differs depending on field of study. The awareness of women using contraception was higher than women which didn’t use hormonal contraception. Conclusion. General state of knowledge of studied women concerning using hormonal contraception was not satisfactory. Especially alarming is ignorance of health threads connected with using hormonal contraception among women using this method of contraception.